Search Result
Results for "
castration
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-19319
-
|
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Epigenetic Reader Domain
Androgen Receptor
Apoptosis
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Cancer
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MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors .
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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-13699
-
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GnRH Receptor
PERK
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Others
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NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca 2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases .
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-
-
- HY-109070
-
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EPI-002
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Androgen Receptor
|
Cancer
|
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Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .
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-
-
- HY-115282A
-
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TRC-253
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Androgen Receptor
|
Cancer
|
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JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
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-
-
- HY-138557
-
|
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17β-HSD
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Cancer
|
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AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research .
|
-
-
- HY-112257
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S-23
1 Publications Verification
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Androgen Receptor
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Metabolic Disease
|
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S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats .
|
-
-
- HY-N0790
-
Lupeol
3 Publications Verification
Clerodol; Monogynol B; Fagarasterol
|
Androgen Receptor
Apoptosis
|
Cancer
|
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Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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-
-
- HY-115282
-
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TRC-253 free base
|
Androgen Receptor
|
Cancer
|
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JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
|
-
-
- HY-N0790R
-
|
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Androgen Receptor
Apoptosis
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Cancer
|
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Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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-
-
- HY-143535
-
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Androgen Receptor
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Cancer
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HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.
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-
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- HY-70006
-
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TOK-001; VN-124-1
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Cytochrome P450
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Cancer
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Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
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-
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- HY-15194
-
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ASC-J9; GO-Y025
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Androgen Receptor
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Cancer
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Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
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-
-
- HY-111503
-
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Epigenetic Reader Domain
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Cancer
|
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Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM .
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-
-
- HY-152512
-
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Androgen Receptor
|
Cancer
|
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RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
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-
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- HY-152520
-
|
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Androgen Receptor
|
Cancer
|
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RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
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-
-
- HY-149927
-
|
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Others
|
Cancer
|
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Antitumor agent-91 is a cyclic phosphate ester derivative with anticancer and anti-proliferative activities. Antitumor agent-91 has potential application in human castration resistant prostate cancer and pancreatic cancer .
|
-
-
- HY-19833
-
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Cytochrome P450
|
Cancer
|
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CFG920 is an orally active, nonsteroidal, reversible dual CYP17 and CYP11B2 inhibitor. CFG920 has the potential for metastatic castration-resistant prostate cancer research .
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-
-
- HY-128938
-
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ADC Linker
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Cancer
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EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC) .
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-
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- HY-125170
-
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STAT
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Cancer
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Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer .
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-
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- HY-128938A
-
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ADC Linker
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Cancer
|
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EC1167 hydrochloride is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 hydrochloride has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC) .
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-
-
- HY-137193
-
|
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Drug Metabolite
|
Cancer
|
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5,6-Dihydroabiraterone is the metabolism of Abiraterone (HY-70013). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, and shows antitumor activity in CRPC (castration-resistant prostate cancer) .
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-
-
- HY-10088
-
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ZD4054
|
Endothelin Receptor
Apoptosis
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Endocrinology
Cancer
|
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Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
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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-146397
-
|
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PROTACs
Androgen Receptor
|
Cancer
|
|
TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research .
|
-
-
- HY-10528
-
|
ABR-215050
|
HDAC
|
Cancer
|
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Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .
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-
-
- HY-P99217
-
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AMG 102
|
c-Met/HGFR
|
Cancer
|
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Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
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-
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- HY-109050
-
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GS-5829
|
Epigenetic Reader Domain
|
Cancer
|
|
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research .
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-
-
- HY-P99802
-
|
BAY 2010112; AMG 212
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CD3
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Cancer
|
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Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
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-
-
- HY-139970
-
|
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Androgen Receptor
|
Endocrinology
Cancer
|
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VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
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-
-
- HY-P99714
-
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MGD019
|
PD-1/PD-L1
CTLA-4
|
Cancer
|
|
Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
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-
-
- HY-124573
-
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TH-3424
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DNA Alkylator/Crosslinker
|
Cancer
|
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OBI-3424 (TH-3424) is a proagent that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research .
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-
-
- HY-164552
-
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Apoptosis
Androgen Receptor
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Cancer
|
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ZNU-IMB-Z15 (Compound Z15) is an antagonist and degrader of androgen receptor (AR). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive castration-resistant prostate cancer (CRPC) cell lines and induce their apoptosis, exhibiting anticancer activity both in vivo and in vitro .
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-
- HY-150102
-
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Androgen Receptor
|
Cancer
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EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
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-
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- HY-119001
-
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Others
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Cancer
|
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BKM1644, an acyl-tyrosine bisphosphonate amide derivative, exhibits potent anti-cancer activity. BKM1644 effectively inhibits the proliferation of metastatic, castration-resistant prostate cance (mCRPC) cells. BKM1644 sensitizes mCRPC cells to Docetaxel (HY-B0011) and retards the bone metastatic growth of prostate cance .
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-
-
- HY-163340
-
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Glucocorticoid Receptor
Androgen Receptor
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Cancer
|
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GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo .
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-
-
- HY-117529
-
|
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Cytochrome P450
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Cancer
|
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BMS-351 (compound 18) is a potent, oral active, nonsteroidal CYP17A1 lyase inhibitor with the IC50 values of 19 nM and 4 nM aganist human CYP17A1 and cynomolgus monkeys CYP17A1,respectively. BMS-351 can be used for the study of castration-resistant prostate cancer .
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-
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- HY-10617
-
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AG-014699 phosphate; PF-01367338 phosphate
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PARP
|
Cancer
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Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research .
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-
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- HY-10617A
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Rucaparib
Maximum Cited Publications
38 Publications Verification
AG014699; PF-01367338
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PARP
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Cancer
|
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Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research .
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-
-
- HY-145388
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
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AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
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-
-
- HY-10617D
-
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AG014699 acetate; PF-01367338 acetate
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PARP
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Cancer
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Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research .
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-
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- HY-10617B
-
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AG014699 hydrochloride; PF-01367338 hydrochloride
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PARP
|
Cancer
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Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research .
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-
-
- HY-102003
-
|
AG014699 monocamsylate; PF-01367338 monocamsylate
|
PARP
|
Cancer
|
|
Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research .
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-
-
- HY-102003A
-
|
AG014699 camsylate; PF-01367338 camsylate
|
PARP
|
Cancer
|
|
Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research .
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-
-
- HY-10617C
-
|
AG-014699 tartrate; PF-01367338 tartrate
|
PARP
|
Cancer
|
|
Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research .
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-
-
- HY-153342
-
|
ARV-766
|
PROTACs
Androgen Receptor
|
Cancer
|
|
Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .
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-
-
- HY-10528S
-
|
ABR-215050-d3
|
HDAC
Isotope-Labeled Compounds
|
Cancer
|
|
Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .
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-
-
- HY-161700
-
|
|
Cytochrome P450
|
Cancer
|
|
BMS-737 (compound 33) is a non-steroidal, reversible small molecule inhibitor. BMS-737 exhibits 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase. BMS-737 is designed to inhibit castration-resistant prostate cancer (CRPC) and significantly reduces testosterone levels without significant effects on orrodermal hormone and glucocorticoid levels .
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-
-
- HY-114732
-
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Adrenergic Receptor
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Others
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Procaterol is an oral selective β2 adrenergic receptor agonist. Procaterol inhibits eosinophil migration and the release of eosinophil chemotactic factor from BEAS-2B cells through a cyclic AMP-dependent mechanism. Procaterol has a large dose difference existing between the bronchodilator effect and the anabolic effect in rat, can be used for asthma research in athletes .
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-
-
- HY-100348
-
|
|
Androgen Receptor
PPAR
Apoptosis
|
Cancer
|
|
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
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-
- HY-149894
-
|
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Biochemical Assay Reagents
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Cancer
|
|
MC-1-F2 is a FOXC2 inhibitor that reduces epithelial-mesenchymal transition (EMT) markers in breast cancer cells, suppresses cancer stem cell (CSC) properties and reduces invasiveness in castration-resistant prostate cancer (CRPC) cells. There is a synergistic effect between MC-1-F2 and Docetaxel, which has the potential to be used in combination to study CRPC .
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-
- HY-107534
-
|
|
GnRH Receptor
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Endocrinology
|
|
AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone .
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-
- HY-144636
-
|
|
Atg4
Cathepsin
Phospholipase
Autophagy
|
Cancer
|
|
Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition .
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-
- HY-42424
-
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VHL ligand 2 hydrochloride; E3 ligase Ligand 1
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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-
- HY-112078
-
|
VHL ligand 2; E3 ligase Ligand 1A
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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-
- HY-42424A
-
|
VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride
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Ligands for E3 Ligase
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Cancer
|
|
(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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-
- HY-N6796
-
|
|
Farnesyl Transferase
Ras
Apoptosis
Phospholipase
TNF Receptor
Atg8/LC3
|
Infection
Inflammation/Immunology
Cancer
|
|
Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion .
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-
- HY-100348R
-
|
|
Androgen Receptor
PPAR
Apoptosis
|
Cancer
|
|
EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
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-
- HY-158125
-
|
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PSMA
|
Cancer
|
|
PSMA binder-2 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
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-
- HY-158119A
-
|
|
PSMA
|
Cancer
|
|
PSMA-trillium is a PSMA targeting compound, consisting of a PSMA targeting molecule (PSMA binder), a Macropa chelating molecule, and a group that regulates pharmacokinetics (PK modifier). PSMA-trillium is a non-radioactive form of Actinium-225-PSMA-Trillium (BAY 3563254) with improved PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind Ac through the Macropa chelating molecule, or the radioactive isotope 225Actinium. Actinium-225-PSMA-Trillium is a potent inhibitor of metastatic castration-resistant prostate cancer (mCRPC) .
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-
- HY-158123
-
|
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PSMA
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Cancer
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PSMA binder-1 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or it can be labeled with 225Ac (to obtain Actinium-225-PSMA-Trillium (BAY 3563254)), which has a radioactive killing effect; it can be used as a Macropa chelator for targeted radionuclide therapy (TRT) , has a strong inhibitory effect on metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-158122
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DNA-PK
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Cancer
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Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-158118
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DNA-PK
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Cancer
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Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99217
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AMG 102
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c-Met/HGFR
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Cancer
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Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
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- HY-P99802
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BAY 2010112; AMG 212
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CD3
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Cancer
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Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-P9992
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BAY-2315497; PSMA-TTC
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Inhibitory Antibodies
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Inflammation/Immunology
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Pelgifatamab (BAY-2315497) is a prostate-specific membrane antigen (PSMA) antibody. Pelgifatamab can be covalently linked to a binding moiety of 225Ac and used for metastatic castration-resistant prostate cancer (mCRPC) research .
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- HY-P99714
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MGD019
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PD-1/PD-L1
CTLA-4
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Cancer
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Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
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Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-10528S
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Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .
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