Search Result
Results for "
xenograft tumor model
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-106031
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Topoisomerase
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Cancer
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F-14512 is a targeted cytotoxic compound that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 combines an epipodophyllotoxin core that targets topoisomerase II with a spermine group that acts as a cell delivery vehicle, with improved selectivity for tumor cells. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and demonstrates high potency in multiple human cell lines (median IC50=0.18 μM). In the MX1 breast tumor xenograft model, F-14512 exhibits potent antitumor activity .
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- HY-153364
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PPAR
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Cancer
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FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models .
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- HY-101120
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Epigenetic Reader Domain
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Cancer
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666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model .
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- HY-156566
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
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- HY-146780
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TGF-β Receptor
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Cancer
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TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model .
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- HY-123334
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Porcupine
Wnt
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Cancer
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GNF-1331 (compound 19) is a potent, selective and orally bioavailable porcupine inhibitor (IC50=12 nM). GNF-1331 blocks Wnt ligand secretion and subsequent Wnt signaling activity, and induces significant antitumor effects in the mouse MMTV-WNT1 xenograft tumor model .
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- HY-156457
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EGFR
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Cancer
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EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
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- HY-143402
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Topoisomerase
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Cancer
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Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
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- HY-169422
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 16 (Example 83) is an orally available WRN inhibitor. WRN inhibitor 16 did not induce tumor regression in the SW48 xenograft mouse tumor model.
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- HY-119618
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Endogenous Metabolite
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Cancer
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R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
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- HY-169779
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p62
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Cancer
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PTX80 is an antagonist of p62 with an IC50 value of 31.18 nM. PTX80 reduces tumor volume in an HCT116 colorectal cancer mouse xenograft model .
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- HY-153521
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BCL6
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Cancer
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CCT374705 is an orally active BCL6 inhibitor with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
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- HY-147784
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Btk
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Cancer
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HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
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- HY-155146
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Necroptosis
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Cancer
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Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .
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- HY-118269
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c-Met/HGFR
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Cancer
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OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
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- HY-136447
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ASP4132
1 Publications Verification
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AMPK
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Cancer
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ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
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- HY-P991189
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- HY-153670
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CCR
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Cancer
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IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research .
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- HY-156111
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PROTACs
Androgen Receptor
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Cancer
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ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
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- HY-P99849
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ABT-806
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EGFR
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Cancer
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Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
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- HY-135217
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Apoptosis
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Cancer
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Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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- HY-146615
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TAM Receptor
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Cancer
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Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
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- HY-P99925
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REGN421
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Notch
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Metabolic Disease
Cancer
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Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
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- HY-169928
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DNA/RNA Synthesis
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Cancer
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WRN inhibitor 14 (compound S35) is an orally active WRN inhibitor with anticancer activity. WRN inhibitor 14 results in tumor growth inhibition in the SW48 xenograft model in BALB/c nude mice .
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- HY-164484
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Raf
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Cancer
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IHMT-RAF-128, a highly potent pan-RAF inhibitor. IHMT-RAF-128 shows potent antitumor efficacy in xenograft mouse tumor models without causing any apparent toxicities .
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- HY-15324
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P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
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Syk
Src
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
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Cancer
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PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models . .
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- HY-162892
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Epigenetic Reader Domain
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Cancer
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BRD4-IN-9 is an orally active BRD4 inhibitor with an IC50 value of 9.4 nM. BRD4-IN-9 can suppress tumor growth in a mouse melanoma xenograft model .
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- HY-15323
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P505-15 Hydrochloride
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Syk
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
Src
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Cancer
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PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models .
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- HY-157029S
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Ras
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Cancer
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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Ras
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Cancer
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-131446
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Checkpoint Kinase (Chk)
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Cancer
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Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
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- HY-163133
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PIKfyve
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Cancer
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PIKfyve-IN-3 (compound L22) has a remarkable interaction with PIKfyve kinase with a Kd value of 0.47 nM. PIKfyve-IN-3 has oral activity. PIKfyve-IN-3 inhibits tumor growth in a HeLa xenograft model .
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- HY-170806
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Estrogen Receptor/ERR
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Cancer
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ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model .
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- HY-163076
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Apoptosis
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Others
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Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cell apoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
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- HY-156568A
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PROTACs
Epigenetic Reader Domain
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Cancer
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SMD-3040 TFA is a selective degrader of SMARCA2. SMD-3040 TFA contains SMARCA2/4 ligands, linker and VHL ligands and can be used for PROTAC drug synthesis. SMD-3040 TFA exhibits strong tumor growth inhibition in tumor xenograft models .
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- HY-13659
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NSC 650426
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Antibiotic
Bcl-2 Family
Apoptosis
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Infection
Cancer
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KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice .
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- HY-157847
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STAT
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Cancer
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Phospho-STAT3-IN-2 (compound 4D) is a STAT3 inhibitor that effectively inhibits STAT3 phosphorylation. phospho-STAT3-IN-2 can significantly reduce tumor volume in mouse xenograft tumor models without drug toxicity to other organs and tissues .
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- HY-153306
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PI3K
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Cancer
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RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
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- HY-153499
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Smo
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Cancer
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SMO-IN-4 (Compound 24) is a potent and orally active smoothened antagonist (IC50: 24 nM). SMO-IN-4 has antitumor activity .
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- HY-124628
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Fatty Acid Synthase (FASN)
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Cancer
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IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
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- HY-147208
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YAP
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Cancer
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MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
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- HY-145835
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PERK
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Cancer
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PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
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- HY-155251
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Apoptosis
Bcl-2 Family
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Cancer
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anti-TNBC agent-3 (compound 3g) is an apoptosis inducer with anti-cancer cell proliferation activity. anti-TNBC agent-3 inhibits tumor growth and metastasis in triple-negative breast cancer (TNBC) xenograft models .
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- HY-149297
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PSMA
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Cancer
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PSMA-IN-1 (compound 23) is an inhibitor of PSMA with a Ki value of 2.49 nM. PSMA-IN-1 inhibits tumor growth with high selectivity and specificity in PSMA+ xenograft models. PSMA-IN-1 is a NIR probe (λEX: 620 nm; λEM: 670 nm) used for tumor disappearance. PSMA-IN-1 can be used for research on prostate cancer .
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- HY-161952
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SHP2
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Cancer
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JAB-3312 is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. JAB-3312 has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .
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- HY-16634
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MDM-2/p53
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Cancer
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MI-888 (TFA) is an orally active MDM2-p53 interaction inhibitor with a Ki of 0.44 nM. MI-888 (TFA) can achieve rapid, complete, and sustained tumor regression in a xenograft mouse model of cancer .
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- HY-19981B
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ARQ-087 dihydrochloride
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EGFR
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Cancer
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Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models .
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- HY-19981
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ARQ-087
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FGFR
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Cancer
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Derazantinib (ARQ-087) is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3 nM). Derazantinib inhibits FGFR phosphorylation. Derazantinib inhibits tumor growth in multiple xenograft models .
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- HY-156633
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PC14586
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MDM-2/p53
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Cancer
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Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation .
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- HY-135217R
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Apoptosis
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Cancer
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Apiole (Standard) is the analytical standard of Apiole. This product is intended for research and analytical applications. Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
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- HY-115514A
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BRK
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Cancer
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BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
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- HY-149081
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Estrogen Receptor/ERR
Cytochrome P450
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Cancer
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ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
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- HY-163301
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Reactive Oxygen Species
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Cancer
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Antitumor agent-139 (compound 9b) is a liver - and mitochondria-targeting gold(I) complexe, and produces reactive oxygen species (ROS) and facilitates DNA excretion. Antitumor agent-139 inhibits tumor growth in a patient-derived xenograft model of hepatocellular carcinoma .
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- HY-W013973
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Fungal
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Cancer
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p-Terphenyl is a p-terphenyl that can be isolated from Aspergillus of the genus Thelephora. p-Terphenyl showed significant anti-tumor and anti-metastatic effects in xenograft models of gastric and pancreatic cancer. Derivatives of p-Terphenyl also have anti-inflammatory or anti-proliferative effects .
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- HY-168950
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Annexin A
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Cancer
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ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with cancer cell inhibition activity. ANXA3 degrader 1 displays excellent inhibitory effect in a triple-negative breast cancer (TNBC) tumor xenograft model (TGI = 96%) .
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- HY-149539
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FLT3
RET
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Cancer
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PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
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- HY-400685
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Drug Intermediate
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Cancer
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SMD-3040 intermediate-2 is an intermediate in the synthesis of SMD-3040 (HY-156568). SMD-3040 contains SMARCA2/4 ligands, linker and VHL ligands and is a selective SMARCA2 degrader. MD-3040 can be used for ADC drug synthesis and has strong tumor growth inhibition in tumor xenograft models .
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- HY-P10759
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Peptide-Drug Conjugates (PDCs)
Aminopeptidase
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Cancer
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DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
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- HY-156681A
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PI3K
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Cancer
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(S)-STX-478 is the S-enantiomer of STX-478. STX-478 is a selective inhibitor of PI3Kα mutants, preventing metabolic dysfunction and demonstrating antitumor activity in xenograft mouse models with PI3Kα mutant tumors .
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- HY-117366
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PKC
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Cancer
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PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
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- HY-16405
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DNA Alkylator/Crosslinker
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Cancer
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PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
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- HY-16406
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DNA Alkylator/Crosslinker
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Cancer
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PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A .
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- HY-149480
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PROTACs
Estrogen Receptor/ERR
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Cancer
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ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
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- HY-144361
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Apoptosis
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Cancer
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Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model .
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- HY-153704
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CDK
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Cancer
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CDK4/6-IN-17 (compound 12) is an orally active CDK4/6 inhibitor with IC50 ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model .
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- HY-163192
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ROR
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Cancer
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W6134 is highly potent and selective RORγ covalent inhibitor with IC50 of 0.21 μM. W6134 exhibits superior activity ini nhibiting the proliferation and colony formation and inducing apoptosis. W6134 can be used for the research of cancer .
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- HY-163658
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PARP
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Cancer
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PARP-1-IN-23 (Compound I16 ) is an orally active and selective PARP-1 inhibitor with the IC50 of 12.38 nM. PARP-1-IN-23 inhibits tumor growth in vivo .
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- HY-155032
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P-glycoprotein
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Cancer
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P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .
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- HY-164427
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SHP2
ERK
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Cancer
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SHP2-IN-31 is a SHP2 inhibitor, with IC50s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models .
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- HY-170933
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SGK
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Cancer
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SGK1-IN-6 (compound 12f) is a potent SGK1 inhibitor with an IC50 of 0.39 μM. SGK1-IN-6 suppresses tumor growth in the PC3 xenograft model in BALB/c nude mice without inducing any observable toxicity .
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- HY-P99922
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LAG-3
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Cancer
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Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
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- HY-120663
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Anaplastic lymphoma kinase (ALK)
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Cancer
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KRCA-0713 is an ALK inhibitor with anti-ALK activity. KRCA-0713 showed promising anti-ALK activity in enzyme and cell-based experiments. KRCA-0713 was shown to effectively inhibit ALK-driven tumor growth in H3122 xenograft model studies, similar to the effect of ceritinib .
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- HY-153834
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DNA/RNA Synthesis
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Cancer
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GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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- HY-101119
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Estrogen Receptor/ERR
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Cancer
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GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
|
-
- HY-118911
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors .
|
-
- HY-162001
-
INX-315
1 Publications Verification
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-N0421
-
|
Cinobufagine
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-122650
-
|
|
Autophagy
|
Cancer
|
|
PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
|
-
- HY-153834A
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
|
-
- HY-168587
-
|
|
Others
|
Cancer
|
|
Antitumor agent-189 (Compound DN4) is a potent antitumor agent. Antitumor agent-189 inhibits A498 cells proliferation, adhesion and invasion with an IC50 of 1.94 μM. Antitumor agent-189 also inhibits angiogenesis and tumor growth in the xenograft model of A498 cells .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-P1651B
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 acetate is the acetate salt form of SOR-C13 (HY-P1651). SOR-C13 acetate is an antagonist for transient receptor potential vanilloid 6 (TRPV 6), with an IC50 of 14 nM. SOR-C13 acetate inhibits tumor growth in SKOV-3 xenograft mouse model .
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-13072
-
|
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-12797
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
GF 15 is an inhibitor of centrosomal clustering during cell mitosis, with an EC50 value of 900 nM for inducing multipolar spindles. GF???15 is a derivative of griseofulvin that inhibits tubulin polymerization at concentrations above 25 μM. GF 15 inhibits tumor growth and significantly prolongs survival in mouse xenograft models of human colon cancer and multiple myeloma .
|
-
- HY-150072
-
|
|
PKA
|
Cancer
|
|
DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC) .
|
-
- HY-122664
-
|
|
BRK
|
Cancer
|
|
XMU-MP-2 is a BRK inhibitor with significant inhibitory activity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2 inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
|
-
- HY-149631
-
|
|
HDAC
|
Cancer
|
|
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models .
|
-
- HY-141606
-
|
BAY 94-9343
|
Microtubule/Tubulin
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Anetumab ravtansine (BAY 94-9343) is a selective and highly potent antibody-drug conjugate (ADC) to target maytansinoid tubulin. Anetumab ravtansine consists of a human anti-mesothelin antibody conjugated to the maytansinoid tubulin inhibitor DM4. Anetumab ravtansine shows antitumor efficacy correlated with the amount of mesothelin expressed in patient-derived xenograft tumor models .
|
-
- HY-156618
-
|
ABSK011
|
FGFR
|
Cancer
|
|
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .
|
-
- HY-16999
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
|
-
- HY-168035
-
|
|
Histone Methyltransferase
|
Cancer
|
|
W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
|
-
- HY-150309
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-54 (compound 10w) 是一种泛 PI3K 抑制剂。PI3K-IN-54 对 p110α、p110β、p110δ 的 IC50 值分别为 0.22 nM、1.4 nM 和 0.38 nM。PI3K-IN-54 可用于癌症研究 。
|
-
- HY-131909
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated .
|
-
- HY-161425
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-149 (Compound 3) is an analogue of Echinomycin (HY-106101). Antitumor agent-149 inhibits HIF-1α-mediated transcription. Antitumor agent-149 induces cancer cell apoptosis. Antitumor agent-149 inhibits tumor growth in SW620 xenograft mice model .
|
-
- HY-121490
-
|
|
Apoptosis
|
Cancer
|
|
IMM-02 is a DID-DAD binding inhibitor with activity promoting actin assembly and microtubule stabilization. IMM-02 is able to trigger serum response factor-mediated gene expression and lead to cell cycle arrest and apoptosis. IMM-02 has shown the ability to slow tumor growth in a mouse colon cancer xenograft model .
|
-
- HY-170812
-
|
|
Aurora Kinase
|
Cancer
|
|
BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .
|
-
- HY-170936
-
|
|
FAK
Hippo (MST)
YAP
|
Cancer
|
|
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
|
-
- HY-13072B
-
|
AS-703569 benzoate; R-763 benzoate
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-115908
-
|
|
CDK
Apoptosis
|
Cancer
|
|
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
|
-
- HY-W013973R
-
|
|
Fungal
|
Cancer
|
|
p-Terphenyl (Standard) is the analytical standard of p-Terphenyl. This product is intended for research and analytical applications. p-Terphenyl is a p-terphenyl that can be isolated from Aspergillus of the genus Thelephora. p-Terphenyl showed significant anti-tumor and anti-metastatic effects in xenograft models of gastric and pancreatic cancer. Derivatives of p-Terphenyl also have anti-inflammatory or anti-proliferative effects .
|
-
- HY-165421
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-10 (Compound 9) is an inhibitor for Mps1 with an IC50 of 6.4 nM. Mps1-IN-10 inhibits the proliferation of cancer cell MDA-MB-231 with a GI50 of 11 nM. Mps1-IN-10 exhibits anti-tumor efficacy in mice MDA-MB-231 xenograft models .
|
-
- HY-168934
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KWR137 is a WRN degrader, with an IC50 of 8 nM. KWR137 exhibits good anti-proliferative activity against MSI-H cells, with a GI50 of 509 nM in SW48 cells and a GI50 of 824 μM in HCT116 cells. It also demonstrates anti-tumor growth effects in xenograft mouse models. KWR137 can be used for cancer research .
|
-
- HY-119062
-
|
|
MetAP
|
Cardiovascular Disease
Cancer
|
|
A-800141 is an orally active and selective MetAP2 inhibitor with an IC50 of 12 nM. A-800141 has weak inhibitory activity for MetAP1 (IC50 : 36 μM). GAPDH can be used as a biomarker to monitor the MetAP2 inhibition of A-800141. A-800141 has antiangiogenic and anticancer activity in a variety of xenograft tumor models .
|
-
- HY-106963
-
|
LGD1550
|
RAR/RXR
|
Cancer
|
|
ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
|
-
- HY-100591
-
|
|
Sirtuin
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
|
-
- HY-117991
-
|
|
VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
|
-
- HY-156568
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models .
|
-
- HY-162010
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile.
MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors treatment research .
|
-
- HY-125065
-
|
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
|
-
- HY-172454
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-36 (Compound B8) is an allosteric inhibitor of SHP2, with an IC50 value of 9.0 nM. In addition, its IC50 for p-ERK is 40 nM. SHP2-IN-36 also exhibited significant antitumor activity in the KYSE520 xenograft mouse model. SHP2-IN-36 can be used for research in the field of anti-tumor .
|
-
- HY-128355A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Others
Cancer
|
|
(R)-IDO/TDO-IN-1 (compound 25) is an indoleamine-2,3-dioxygenase (IDO) inhibitor, with good pharmacokinetic properties. (R)-IDO/TDO-IN-1 exhibits anti-tumor activity in MC38 xenograft model. (R)-IDO/TDO-IN-1 shows synergistic effect with anti-PD-1 monoclonal antibody (SHR-1210) .
|
-
- HY-15772R
-
|
|
EGFR
|
Cancer
|
|
Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-15772AR
-
|
|
EGFR
|
Cancer
|
|
Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-15772S
-
|
AZD-9291-d6; Mereletinib-d6
|
EGFR
|
Cancer
|
|
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
|
-
- HY-15772
-
Osimertinib
Maximum Cited Publications
122 Publications Verification
AZD-9291; Mereletinib
|
EGFR
|
Cancer
|
|
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-162230
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity .
|
-
- HY-15772A
-
|
AZD-9291 mesylate; Mereletinib mesylate
|
EGFR
|
Cancer
|
|
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-169310
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
|
-
- HY-151462
-
RP-6685
1 Publications Verification
|
DNA/RNA Synthesis
|
Cancer
|
|
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model . RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N0421R
-
|
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
|
-
- HY-150636
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-172175
-
|
|
mTOR
Akt
PI3K
Apoptosis
Autophagy
|
Cancer
|
|
HYS-072 is an orally active derivative of chrysin (HY-14589) with antitumor activity. HYS-072 induces apoptosis and autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway and suppresses tumor growth in vivo in xenograft models by modulating autophagy-related pathways. HYS-072 can be used in the research of triple-negative breast cancer .
|
-
- HY-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-165245
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
|
-
- HY-123045
-
|
|
CDK
|
Cancer
|
|
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
|
-
- HY-P5520
-
|
|
Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
|
-
- HY-13440
-
AMG 511
2 Publications Verification
|
PI3K
|
Cancer
|
|
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
|
-
- HY-167876
-
|
|
PI3K
|
Cancer
|
|
PQR514 is a potent PI3K inhibitor with anticancer activity. PQR514 is able to inhibit cancer cell proliferation. PQR514 showed significant antitumor activity in the OVCAR-3 xenograft model, with the required concentration being approximately one-eighth that of PQR309. PQR514 has good pharmacokinetic properties and minimal brain penetration, making it an optimized candidate compound for inhibiting systemic tumors .
|
-
- HY-150023
-
|
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-146114
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity .
|
-
- HY-169937
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .
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-
- HY-110077
-
API-1
1 Publications Verification
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Akt
Apoptosis
Caspase
PARP
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Cancer
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|
API-1 is a potent selective Akt/PKB inhibitor that reduces the level of phosphorylated Akt (IC50 = 0.8 μM). API-1 binds to the PH domain and inhibits Akt membrane translocation. API-1 induces c-FLIP degradation. API-1 reduces cell proliferation and induces apoptosis. API-1 decreases tumor growth in mouse xenograft model .
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-
- HY-162881
-
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EGFR
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Cancer
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DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI50 value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .
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- HY-155532
-
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Apoptosis
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Cancer
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10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
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-
- HY-146462
-
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Apoptosis
ROS Kinase
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Cancer
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Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
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-
- HY-131328
-
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LOXO-305
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Btk
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Cancer
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|
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
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- HY-117707
-
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Raf
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Cancer
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EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
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- HY-P990027
-
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ADC Antibody
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Cancer
|
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Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
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- HY-12965B
-
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TAM Receptor
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Cancer
|
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(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
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-
- HY-146323
-
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Apoptosis
|
Cancer
|
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Antitumor agent-58 (Compound C18) is an anti-tumor agent. Antitumor agent-58 effectively inhibits colony formation and cell migration of MGC-803 cells. Antitumor agent-58 induces apoptosis of MGC-803 cells through activation of the p38 and JNK signaling pathways. Antitumor agent-58 induces mitochondrial dysfunction of MGC-803 cells. Antitumor agent-58 effectively inhibits tumor growth of xenograft model bearing MGC-803 cells .
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-
- HY-155356
-
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PROTACs
Ras
|
Cancer
|
|
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
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-
- HY-P10761
-
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Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
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Cancer
|
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DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130?nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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-
- HY-170764
-
|
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YAP
|
Cancer
|
|
M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC50 value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC50 value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model .
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-
- HY-W998345
-
|
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PROTACs
PDK-1
Akt
|
Cancer
|
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .
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-
- HY-155489
-
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Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
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DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
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-
- HY-103441
-
|
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EGFR
|
Cancer
|
|
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
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-
- HY-157317
-
|
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Apoptosis
|
Cancer
|
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Antitumor agent-126 (Compound II4) is a photoactive (IC50= 0.149) anticancer agent with significant near-infrared fluorescence emission at 650-760 nm. Antitumor agent-126 has antiproliferative activity and can induce apoptosis after laser irradiation. Antitumor agent-126 effectively inhibits tumor growth in mouse xenograft models exposed to 650 nm laser irradiation. Antitumor agent-126 can be used in cancer research .
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-
- HY-12757
-
|
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BCRP
|
Cancer
|
|
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
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-
- HY-169078
-
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Histone Methyltransferase
|
Cancer
|
|
ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
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-
- HY-P99272
-
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BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
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CXCR
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Cancer
|
|
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .
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-
- HY-15186
-
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GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
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-
- HY-161629
-
|
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Toll-like Receptor (TLR)
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Cancer
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TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98% .
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-
- HY-168899
-
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FAK
Apoptosis
|
Cancer
|
|
FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC50: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC50 = 15 nM) and U251 (IC50 = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model .
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-
- HY-15186C
-
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GDC-0068 tosylate; RG7440 tosylate
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
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-
- HY-169120
-
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Telomerase
|
Cancer
|
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FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research .
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-
- HY-139061
-
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LPL Receptor
ROCK
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Cancer
|
|
Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
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-
- HY-117938
-
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Aminoacyl-tRNA Synthetase
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Cancer
|
|
T-3861174 is an inhibitor of prolyl-tRNA synthetase (PRS, Aminoacyl-tRNA Synthetase) without completely inhibiting its translation process. T-3861174 activates the GCN2-ATF4 pathway and induces death in multiple tumor cell lines, including SK-MEL-2. T-3861174 demonstrated significant antitumor activity in multiple xenograft models without significantly affecting body weight .
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-
- HY-168300
-
|
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Reactive Oxygen Species
Apoptosis
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Inflammation/Immunology
Cancer
|
|
Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models .
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-
- HY-123972
-
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KL-2
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DNA/RNA Synthesis
|
Cancer
|
|
SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM .
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-
- HY-143471
-
|
PLK1/BRD4-IN-1
|
Polo-like Kinase (PLK)
Epigenetic Reader Domain
Apoptosis
Androgen Receptor
c-Myc
|
Cancer
|
|
WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .
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-
- HY-161630
-
|
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Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89% .
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-
- HY-160962
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
SM1044 is a dihydroartemisinin (DHA) dimer. SM1044 activates caspase, induces apooptosis in RL95-2 and KLE cells. SM1044 inhibits proliferations of cancer cells RL95-2, KLE, HEC-50, HEC-1-A, HEC-1-B, AN3CA, with IC50 < 3.6 μM . SM1044 inhbits tumor growth in RL95-2 xenograft mouse model .
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-
- HY-144777
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
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-
- HY-169002
-
|
|
Phosphatase
|
Cancer
|
|
PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC50 value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .
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-
- HY-149695
-
|
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EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
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-
- HY-137849
-
|
|
PARP
|
Cancer
|
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
|
-
- HY-161631
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97% .
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-
- HY-149677
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
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-
- HY-146494
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
|
-
- HY-P10744
-
|
|
Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-159577
-
|
|
PI3K
mTOR
Akt
|
Cancer
|
|
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
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-
- HY-163612
-
|
|
ROR
Apoptosis
|
Cancer
|
|
XY077 (compound 14a) is a RORγ inverse agonist with the IC50 of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
|
-
- HY-163611
-
|
|
ROR
|
Cancer
|
|
XY039 (compound 13e) is a RORγ inverse agonist with the IC50 of 0.55 μM. XY039 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
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-
- HY-149410
-
|
|
Topoisomerase
|
Cancer
|
|
MSN8C, an analog of mansonone E, is a novel catalytic inhibitor of human DNA topoisomerase II. MSN8C induces cancer cell apoptosis. MSN8C shows significant anti-tumor cell proliferation activity in vitro .
|
-
- HY-148813
-
|
|
PROTACs
STAT
|
Cancer
|
|
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-164689
-
|
|
Proteasome
|
Cancer
|
|
Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .
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-
- HY-146755
-
|
|
Trk Receptor
|
Cancer
|
|
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
|
-
- HY-169075
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC50 values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .
|
-
- HY-151263
-
|
|
HDAC
G-quadruplex
|
Cancer
|
|
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer .
|
-
- HY-146461
-
|
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
|
-
- HY-156077
-
|
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
anti-TNBC agent-2 (3j) an anti-Triple negative breast cancer (TNBC) purine derivative. anti-TNBC agent-2 induces MDA-MB-231 cells apoptosis, and inhibits its migration and angiogenesis. anti-TNBC agent-2 inhibits tumor growth and metastasis and reduces the expression of Ki67 and CD31 protein in TNBC xenograft models. anti-TNBC agent-2 can be used for Triple negative breast cancer (TNBC) research .
|
-
- HY-139659
-
|
|
PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
|
Cancer
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-162688
-
|
|
Telomerase
G-quadruplex
Apoptosis
Ferroptosis
|
Others
|
|
Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model .
|
-
- HY-121365
-
|
|
Bacterial
|
Infection
|
|
Forphenicinol is an immunomodulator and a derivative of the bacterial metabolite forphenicine. It increases the phagocytosis of yeast by peritoneal macrophages isolated from thioglycolate-stimulated mice. Forphenicinol (100 μg/animal) prevents cyclophosphamide-induced suppression of delayed-type hypersensitivity (DTH), as well as enhances DTH in response to the hapten oxazolone or sheep red blood cells in mice. It enhances the bactericidal activity of macrophages against P. aeruginosa in mice when administered at a dose of 0.5 mg/kg.2 Forphenicinol (15.6-1,000 μg/animal) increases survival in a mouse model of P. aeruginosa infection. It also inhibits tumor growth in S180 sarcoma and IMC carcinoma mouse xenograft models when administered at doses ranging from 0.05 to 5 mg/kg per day.
|
-
- HY-149427
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
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- HY-146432
-
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Apoptosis
Raf
Ras
ROS Kinase
MDM-2/p53
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Cancer
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Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
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-
- HY-162873
-
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MEK
Raf
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Cancer
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|
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
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- HY-170855A
-
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PROTACs
RET
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Cancer
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|
YW-N-7 (TFA) is a PROTAC that targets both the inhibition and degradation of RET kinase, with a DC50 of 88 nM. YW-N-7 (TFA) exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse tumor model and can be used in the area of cancer (Structure: red part represents the target protein ligand: HY-170856; blue part represents the E3 ligase ligand: HY-1708557; black part represents the linker; E3 ligase ligand + linker: HY-170858) .
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- HY-155226
-
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FLT3
Apoptosis
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Cancer
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|
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
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- HY-169349
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Androgen Receptor
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Cancer
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|
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
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- HY-111790
-
M3258
1 Publications Verification
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Proteasome
Apoptosis
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Cancer
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M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
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- HY-159803
-
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6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin
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Endogenous Metabolite
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Cancer
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IST-622 (6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin) is an anti-tumor agent with significant growth inhibitory activity. IST-622 exhibits significant anti-tumor effects against a variety of mouse tumors such as P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, Colon 26 and Colon 38 adenocarcinomas, and M5076 reticulum cell sarcoma. IST-622 was orally administered and the results showed efficacy in different tumor types. In addition, IST-622 provided significant inhibitory effects against two human tumor xenograft models: large cell lung carcinoma (Lu-116) and gastric adenocarcinoma (St-4). IST-622 also exhibited significant growth inhibitory activity against P388 leukemia in vitro, with a half inhibitory concentration (IC50) more than 20 times lower than CT .
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-
- HY-160506
-
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PROTACs
c-Met/HGFR
Apoptosis
|
Cancer
|
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PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .
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- HY-150538
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STAT
Apoptosis
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Cancer
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STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. STAT3-IN-12 inhibits cancer cell growth, migration, and induce cell apoptosis as well as cycle arrest. STAT3-IN-12 can be used in cancer-related research, such as hepatocellular carcinoma (HCC) and oesophageal carcinoma .
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-
- HY-168555
-
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CDK
PROTACs
Apoptosis
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Cancer
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YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
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- HY-123237
-
|
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c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
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Cancer
|
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KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
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-
- HY-W276819
-
|
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Polo-like Kinase (PLK)
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Cancer
|
|
PLK1-IN-9 (Compound M2) is an inhibitor for polo-like kinase 1 (PLK1), that inhibits PLK proteins modified with peptides 1010pT, cdc25c and PBIP, with IC50s of 1.6, 0.8 and 1.4 μM, respectively. PLK1-IN-9 inhibits proliferations of cancer cells HeLa, HL60, SNU387/499, HepG2, exhibits cytotoxicity and induces apoptosis. PLK1-IN-9 inhibits tumor growth in HepG2 xenograft mouse model .
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-
- HY-P99744
-
|
TAK-573
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CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
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-
- HY-170947
-
|
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STAT
Quinone Reductase
|
Cancer
|
|
Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
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-
- HY-126287
-
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Trk Receptor
Apoptosis
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Cancer
|
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
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-
- HY-149295
-
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PROTACs
Estrogen Receptor/ERR
Apoptosis
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Cancer
|
|
PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER + breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
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-
- HY-163527
-
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FGFR
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Cancer
|
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
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- HY-155993
-
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PARP
|
Cancer
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|
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats .
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- HY-149433
-
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Androgen Receptor
Apoptosis
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Cancer
|
|
BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
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-
- HY-155066
-
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PI3K
mTOR
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
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-
- HY-156792
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Ser/Thr Kinase
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Cancer
|
|
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
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-
- HY-169830
-
|
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Drug Derivative
Apoptosis
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Cancer
|
|
2-(Cyclohexylmethyl)-plumbagin is a derivative of the naphthoquinone compound Plumbagin (HY-N1497). Under nutrient-deprived conditions, 2-(Cyclohexylmethyl)-plumbagin selectively exhibits cytotoxicity against PANC-1 human pancreatic cancer cells (PC50 = 0.11 µM) and reduces the phosphorylation of Akt and mTOR in PANC-1 cells. 2-(Cyclohexylmethyl)-plumbagin also induces apoptosis (Apoptosis) in PANC-1 cells at a concentration of 1 µM. Additionally, 2-(Cyclohexylmethyl)-plumbagin reduces tumor volume and weight in a xenograft MiaPaCa-2 pancreatic cancer mouse model .
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-
- HY-148409
-
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Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
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Cancer
|
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MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
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-
- HY-150613
-
|
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Epigenetic Reader Domain
PARP
Apoptosis
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Cancer
|
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
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-
- HY-143881
-
|
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FGFR
|
Cancer
|
|
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-164411
-
|
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c-Met/HGFR
|
Cancer
|
|
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
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-
- HY-153321
-
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BTK-IN-24
|
Btk
PROTACs
|
Inflammation/Immunology
Cancer
|
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
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- HY-144099
-
|
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E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity .
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-
- HY-147259
-
|
|
c-Met/HGFR
|
Cancer
|
|
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
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-
- HY-160777
-
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Galeterone 3β-imidazole
|
Molecular Glues
Androgen Receptor
MNK
|
Cancer
|
|
VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
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-
- HY-121081
-
|
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CDK
|
Cancer
|
|
BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
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-
- HY-158156
-
|
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NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models .
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-
- HY-170968
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC50 of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .
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-
- HY-123929
-
|
|
MDM-2/p53
Wnt
IKK
Apoptosis
Caspase
|
Cancer
|
|
PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model .
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-
- HY-168715
-
|
|
SHP2
Apoptosis
MAPKAPK2 (MK2)
|
Cancer
|
|
SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC50 of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC50 of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .
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-
- HY-P10819
-
|
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Histone Demethylase
Apoptosis
|
Cancer
|
|
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
|
-
- HY-157228
-
|
|
PROTACs
Ras
|
Cancer
|
|
ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
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-
- HY-156110
-
|
|
Insulin Receptor
|
Cancer
|
|
IGF2BP1-IN-1 (Compound A11) is a IGF2BP1 inhibitor and inhibits downstream signaling. IGF2BP1-IN-1 binds to IGF2BP1 protein with a KD value of 2.88 nM. IGF2BP1-IN-1 inhibits cancer cells proliferation (IC50: 9 nM for A549 cell, 34 nM for HCT116). IGF2BP1-IN-1 induces cancer cell apoptosis. GF2BP1-IN-1 inhibits tumor growth in A549 xenograft mouse model .
|
-
- HY-158726
-
|
|
Fluorescent Dye
|
Cancer
|
|
Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume and intratumor apoptosis in an AsPC-1 mouse xenograft model .
|
-
- HY-173147
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 value of 10 nM. CDK2-IN-42 has anti-ESCC (Esophageal Squamous Cell Carcinoma) cell activity. It can block transcriptional elongation, downregulate the core genes in the G1 phase to induce cell cycle arrest, and alter the CDK12-ATM/ATR-CHEK1/CHEK2 signaling axis, resulting in DNA damage. CDK2-IN-42 can effectively inhibit tumor growth in a xenograft mouse model of human ESCC KYSE150. CDK2-IN-42 holds great promise for research in the field of cancer .
|
-
- HY-159912
-
|
|
YAP
|
Cancer
|
|
pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
|
-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-164490
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
|
-
- HY-139062
-
|
C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
|
Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
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-
- HY-146095
-
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MDM-2/p53
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
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-
- HY-162704
-
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PROTACs
|
Cancer
|
|
JMV7048 is an effective PROTAC degrader targeting PXR (Pregnane X Receptor) with a DC50 of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker) .
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- HY-159922
-
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Androgen Receptor
|
Cancer
|
|
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
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- HY-167854
-
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Aurora Kinase
Apoptosis
IGF-1R
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Cancer
|
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KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
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- HY-163985
-
|
|
PROTACs
FGFR
Apoptosis
|
Cancer
|
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PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) .
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-
- HY-170824
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
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SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827) .
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- HY-136765
-
|
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PI3K
|
Cancer
|
|
PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
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| Cat. No. |
Product Name |
Type |
-
- HY-158726
-
|
|
Fluorescent Dyes/Probes
|
|
Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume and intratumor apoptosis in an AsPC-1 mouse xenograft model .
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| Cat. No. |
Product Name |
Type |
-
- HY-W013973
-
|
|
Biochemical Assay Reagents
|
|
p-Terphenyl is a p-terphenyl that can be isolated from Aspergillus of the genus Thelephora. p-Terphenyl showed significant anti-tumor and anti-metastatic effects in xenograft models of gastric and pancreatic cancer. Derivatives of p-Terphenyl also have anti-inflammatory or anti-proliferative effects .
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- HY-W013973R
-
|
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Biochemical Assay Reagents
|
|
p-Terphenyl (Standard) is the analytical standard of p-Terphenyl. This product is intended for research and analytical applications. p-Terphenyl is a p-terphenyl that can be isolated from Aspergillus of the genus Thelephora. p-Terphenyl showed significant anti-tumor and anti-metastatic effects in xenograft models of gastric and pancreatic cancer. Derivatives of p-Terphenyl also have anti-inflammatory or anti-proliferative effects .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1651B
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 acetate is the acetate salt form of SOR-C13 (HY-P1651). SOR-C13 acetate is an antagonist for transient receptor potential vanilloid 6 (TRPV 6), with an IC50 of 14 nM. SOR-C13 acetate inhibits tumor growth in SKOV-3 xenograft mouse model .
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- HY-P10759
-
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Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
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- HY-P5520
-
|
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Bombesin Receptor
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects .
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- HY-P10761
-
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Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130?nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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-
- HY-P10744
-
|
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Radionuclide-Drug Conjugates (RDCs)
PSMA
|
Cancer
|
|
BQ7859 is a probe targeting PSMA that contains a NOTA chelator and demonstrates excellent imaging performance. BQ7859 can be labeled with various radionuclides, such as 68Ga, 18F, 55Co, and 111In. In a mouse prostate cancer xenograft model, BQ7859 (labeled with 111In) efficiently accumulates in tumor regions in a PSMA-dependent manner and provides high-contrast tumor imaging. BQ7859 shows potential for research in prostate cancer imaging, particularly in positron emission tomography (PET) and single-photon emission computed tomography (SPECT) . BQ7859 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-P10819
-
|
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Histone Demethylase
Apoptosis
|
Cancer
|
|
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99849
-
|
ABT-806
|
EGFR
|
Cancer
|
|
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
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-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
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-
- HY-P99922
-
|
|
LAG-3
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
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-
- HY-P990027
-
|
|
ADC Antibody
|
Cancer
|
|
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
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-
- HY-P99272
-
|
BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
|
CXCR
|
Cancer
|
|
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .
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-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
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-
- HY-P99275
-
|
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
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-
- HY-P991189
-
-
- HY-141606
-
|
BAY 94-9343
|
Microtubule/Tubulin
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Anetumab ravtansine (BAY 94-9343) is a selective and highly potent antibody-drug conjugate (ADC) to target maytansinoid tubulin. Anetumab ravtansine consists of a human anti-mesothelin antibody conjugated to the maytansinoid tubulin inhibitor DM4. Anetumab ravtansine shows antitumor efficacy correlated with the amount of mesothelin expressed in patient-derived xenograft tumor models .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-157029S
-
|
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
-
- HY-157031S
-
|
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
-
- HY-15772S
-
|
|
|
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-157029S
-
|
|
|
Alkynes
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-157031S
-
|
|
|
Alkynes
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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| Cat. No. |
Product Name |
|
Classification |
-
- HY-153834
-
|
|
|
Aptamers
|
|
GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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-
- HY-153834A
-
|
|
|
Aptamers
|
|
GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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