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Cat. No. Product name CAS No.
DC11908 Ralaniten

A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer.

DC11909 Ralaniten acetate

A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer.

DC11544 Onapristone

A synthetic, steroidal progesterone receptor (PR) antagonist with reduced antiglucocorticoid activity compared to mifepristone..

DC11452 ABBV-744 Featured

ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.BBV-744, a highly potent and selective inhibitor of the BD2 domain of BET family proteins with drug-like properties. In contrast to the broad range of cell growth inhibition induced by DbBi, the antiproliferative activity of ABBV-744 was largely, but not exclusively, restricted to cell lines of acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR). ABBV-744 retained robust activity in prostate cancer xenografts, and showed fewer platelet and gastrointestinal toxicities than the DbBi ABBV-07514.Analyses of RNA expression and chromatin immunoprecipitation followed by sequencing revealed that ABBV-744 displaced BRD4 from AR-containing super-enhancers and inhibited AR-dependent transcription, with less impact on global transcription compared with ABBV-075. These results underscore the potential value of selectively targeting the BD2 domain of BET family proteins for cancer therapy.

DC2710 Abiraterone (CB-7598)

Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM.

DC7056 AMG-208 Featured

AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.

DC10588 ASP-9521 Featured

ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.

DC7460 Masitinib Featured

Masitinib is a broad coronavirus 3CL inhibitor that effectively blocks replication of SARS-CoV-2. Science 20 Jul 2021: eabg5827 DOI: 10.1126/science.abg5827

DC5069 Enzalutamide (MDV3100) Featured

MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

DC8700 ODM-201(Darolutamide) Featured

ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.

DC7160 SGI-1776 Featured

SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM; 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin.

DC7733 Tasquinimod(ABR-215050) Featured

Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling.

DC8008 TOK-001(Galeterone) Featured

TOK-001 is a multifunctional antiandrogen and CYP17 inhibitor(IC50=47 nM) in castration resistant prostate cancer (CRPC).

DC9435 Zibotentan(ZD4054) Featured

Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).

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