Search Result
Results for "
regression
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-114277
-
Sotorasib
Maximum Cited Publications
57 Publications Verification
AMG-510
|
Ras
|
Cancer
|
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors .
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-
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- HY-13479
-
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HSP
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Cancer
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EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases . EC144 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-145734A
-
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Microtubule/Tubulin
|
Cancer
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AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors .
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-
-
- HY-145734
-
|
Microtubule/Tubulin
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Cancer
|
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .
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-
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- HY-160047
-
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PDGFR
|
Cancer
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AX102 sodium is a 34 bp length nucleotide aptamer modified at the 5' end with a 40 kDa polyethylene glycol moiety. AX102 selectively binds platelet-derived growth factor B (PDGF-B) and causes tumor vessel regression .
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-
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- HY-160048
-
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PDGFR
|
Cancer
|
PEG40K unconjugated/naked AX102 sodium is AX102 without PEG40K conjugation. AX102 is a DNA oligonucleotide aptamer for platelet-derived growth factor PDGF-B. AX102 is 34 bases in length, selectively binds platelet-derived growth factor B (PDGF-B), and causes tumor vessel regression .
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-
-
- HY-120264
-
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Others
|
Cancer
|
YPC-22026 is a zinc-finger protein 143 (ZNF143) inhibitor with an IC50 value of 9.0 μM. YPC-22026 is a potent tumor regression inducer. YPC-22026 exhibits anti‐tumor activities .
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-
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- HY-162881
-
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EGFR
|
Cancer
|
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-161373
-
|
PI3K
|
Cancer
|
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .
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-
-
- HY-117707
-
|
Raf
|
Cancer
|
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-148029
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TAK-676
|
STING
|
Cancer
|
Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity .
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-
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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-164490
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EGFR
Apoptosis
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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 .
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- HY-132234
-
|
Epigenetic Reader Domain
|
Cancer
|
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression .
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-
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- HY-132922
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APG-5918
|
Histone Methyltransferase
|
Cancer
|
EEDi-5273 is an exceptionally potent and orally efficacious EED inhibitor (IC50 = 0.2 nM) capable of achieving complete and persistent tumor regression.
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-
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- HY-W035051
-
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Fluorescent Dye
|
Infection
Cancer
|
TSPP tetrasodium is a photosensitizer that has shown impressive effects in in vivo regression of cancer and microorganism infections (Ex: 413 nm, Em: 640 nm) .
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-
-
- HY-136447
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ASP4132
1 Publications Verification
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AMPK
|
Cancer
|
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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-
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- HY-114228
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
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-
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- HY-12885
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ADU-S100; MIW815; ML RR-S2 CDA
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STING
|
Inflammation/Immunology
Cancer
|
2’3’-c-di-AM(PS)2 (Rp,Rp) (ADU-S100), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity .
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-
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- HY-12885B
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ADU-S100 ammonium salt; MIW815 ammonium salt; ML RR-S2 CDA ammonium salt
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STING
|
Inflammation/Immunology
Cancer
|
2’3’-c-di-AM(PS)2 (Rp,Rp) ammonium salt (ADU-S100 ammonium salt), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity .
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- HY-111145
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|
Androgen Receptor
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Cancer
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RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
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-
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- HY-122315
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NSC-741909
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Others
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Others
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Oncrasin-60 (NSC-741909) is a compound with antitumor activity that is active against multiple cancer cell lines in vitro and can induce tumor regression in vivo, with its mechanism involving JNK activation and STAT3 inhibition.
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-
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- HY-156681
-
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PI3K
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Cancer
|
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .
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-
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- HY-110201
-
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Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
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-
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- HY-151559
-
|
Checkpoint Kinase (Chk)
STAT
CXCR
CCR
|
Cancer
|
Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .
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-
-
- HY-126762
-
|
Progesterone Receptor
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Endocrinology
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Fenprostalene is an analog of Dinoprost (PGF2α) (HY-12956) that is used in veterinary medicine to induce corpus luteum regression and blood Progesterone (HY-N0437) levels reduction in dogs. Fenprostalene is potent in ameliorating pyometra and inducing abortion .
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-
-
- HY-17449
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CA 4DP; CA 4P; Combretastatin A4 disodium phosphate
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent. Fosbretabulin disodium is the Combretastatin A4 proagent that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis .
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-
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- HY-161952
-
|
SHP2
|
Cancer
|
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-147250A
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RLY-4008 hydrochloride
|
FGFR
|
Cancer
|
Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
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-
-
- HY-147250
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RLY-4008
|
FGFR
|
Cancer
|
Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs .
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-
-
- HY-148274
-
|
PROTACs
IRAK
Apoptosis
|
Cancer
|
KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88 MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model .
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-
-
- HY-114277S
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AMG-510-d7
|
Ras
|
Cancer
|
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib is an orally active covalent inhibitor of KRAS G12C. Sotorasib can lead to the regression of KRAS G12C tumors .
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-
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- HY-P99776
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XmAb-13676
|
CD20
CD3
|
Cancer
|
Plamotamab (XmAb-13676) is a human bispecific antibody (bsAb) that binds CD3 and CD20. Plamotamab recruits cytotoxic T cells to kill CD20 + expressing tumor cells. Plamotamab induces a mild hematologic reaction (MR), and results in tumor regression in vivo .
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- HY-10984A
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(S)-CC-4047
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Others
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Cancer
|
(S)-Pomalidomide ((S)-CC-4047) is an angiogenesis-inhibiting drug with growth-inhibitory activity against B-cell tumors. (S)-Pomalidomide can induce complete tumor regression in BurKitt lymphoma cells. (S)-Pomalidomide serves as an immunomodulator with potential applications in inhibiting hematological malignancies .
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- HY-100765
-
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MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
|
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis .
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-
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- HY-144070
-
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Others
|
Cancer
|
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model .
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-
-
- HY-101519
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ZBC 260
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line . BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells .
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-
-
- HY-119257
-
|
Farnesyl Transferase
Apoptosis
|
Cancer
|
ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity .
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-
-
- 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 .
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-
-
- HY-10517A
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(Z)-SU6668; (Z)-TSU-68
|
VEGFR
PDGFR
FGFR
|
Cancer
|
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors .
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-
-
- HY-141523
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RMC-4630; SHP2-IN-7
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SHP2
Phosphatase
|
Cancer
|
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .
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-
-
- HY-16231
-
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Apoptosis
|
Cancer
|
GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors .
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-
-
- HY-155537
-
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EGFR
|
Cancer
|
YK-029A is an orally active inhibitor of mutant EGFR,targeting to both the T790M mutations (EGFR T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity,and results tumor regression in EGFRex20ins-driven PDX models .
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-
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- HY-136360
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MI-3454
2 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis .
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-
-
- HY-114440
-
GR-MD-02
|
Galectin
Apoptosis
|
Cancer
|
Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity Ki of 2.8 μM .
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-
-
- HY-159730
-
|
Others
|
Cancer
|
ERG245 is a BCAT1 inhibitor that enhances oxidative phosphorylation (OXPHOS) in CD8 + T cells by specifically inhibiting BCAT1 activity, thereby increasing the cytotoxicity of CD8 + T cells. ERG245, in combination with Pembrolizumab (anti-PD-1, HY-P9902A), promotes tumor regression. ERG245 can be used in research related to immuno-oncology .
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-
-
- HY-102087
-
JPM-OEt
3 Publications Verification
|
Cathepsin
|
Cancer
|
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .
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-
-
- HY-111373
-
|
mTOR
Autophagy
|
Cancer
|
RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity .
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-
-
- HY-131328
-
LOXO-305
|
Btk
|
Cancer
|
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-168555
-
|
CDK
PROTACs
Apoptosis
|
Cancer
|
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 .
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-
- HY-136927
-
|
STING
|
Inflammation/Immunology
Cancer
|
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
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-
- HY-145414
-
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Others
|
Cancer
|
DYSP-C34 is a potent, biocompatible, and ultrasound (US)-triggered multifunctional molecular machine. DYSP-C34 has multiple favorable properties, such as improved lipophilic/hydrophilic balance, intensified US-induced ROS production capacity, and better cellular permeability, resulting in the excellent tumor target efficiency and notable sonodynamic therapy (SDT)-mediated tumor regression. DYSP-C34 exhibits mild immunogenicity by stimulating APCs directly .
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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-168088
-
|
HDAC
DNA Methyltransferase
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Cancer
|
DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .
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-
- 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.
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-
- HY-150725
-
|
IFNAR
TNF Receptor
|
Infection
Inflammation/Immunology
Cancer
|
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
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-
- 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-155356
-
|
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-150725C
-
|
TNF Receptor
IFNAR
|
Cancer
|
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 sodium can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
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-
- HY-156498
-
|
Ras
ERK
Raf
Ribosomal S6 Kinase (RSK)
AMPK
Apoptosis
PARP
|
Cancer
|
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
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-
- HY-168012
-
|
Ras
Phosphatase
|
Cancer
|
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
|
-
- HY-129602
-
SD-36
5 Publications Verification
|
PROTACs
STAT
Apoptosis
|
Cancer
|
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 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-118899
-
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Others
|
Cancer
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XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
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Cat. No. |
Product Name |
Type |
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- HY-W035051
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Biochemical Assay Reagents
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TSPP tetrasodium is a photosensitizer that has shown impressive effects in in vivo regression of cancer and microorganism infections (Ex: 413 nm, Em: 640 nm) .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99776
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XmAb-13676
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CD20
CD3
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Cancer
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Plamotamab (XmAb-13676) is a human bispecific antibody (bsAb) that binds CD3 and CD20. Plamotamab recruits cytotoxic T cells to kill CD20 + expressing tumor cells. Plamotamab induces a mild hematologic reaction (MR), and results in tumor regression in vivo .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-114277S
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Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib is an orally active covalent inhibitor of KRAS G12C. Sotorasib can lead to the regression of KRAS G12C tumors .
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Cat. No. |
Product Name |
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Classification |
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- HY-150725C
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CpG ODNs
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ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 sodium can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
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- HY-160047
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Aptamers
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AX102 sodium is a 34 bp length nucleotide aptamer modified at the 5' end with a 40 kDa polyethylene glycol moiety. AX102 selectively binds platelet-derived growth factor B (PDGF-B) and causes tumor vessel regression .
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- HY-160048
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Aptamers
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PEG40K unconjugated/naked AX102 sodium is AX102 without PEG40K conjugation. AX102 is a DNA oligonucleotide aptamer for platelet-derived growth factor PDGF-B. AX102 is 34 bases in length, selectively binds platelet-derived growth factor B (PDGF-B), and causes tumor vessel regression .
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- HY-150725
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CpG ODNs
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ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
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