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Chemical Structure : BMS-986365
CAS No.: 2446928-30-7
Catalog No.: PC-22117Not For Human Use, Lab Use Only.
BMS-986365 (CC-94676) is a highly potent and selective androgen receptor (AR) degrader with DC50 of 10-40 nM, induces rapid and deep degradation of both wildtype and mutant forms of AR.
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|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $548 | In stock | |
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| 100 mg | Get quote |
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BMS-986365 (CC-94676) is a highly potent and selective androgen receptor (AR) degrader with DC50 of 10-40 nM, induces rapid and deep degradation of both wildtype and mutant forms of AR.
BMS-986365 is a heterobifunctional ligand-directed degrader (LDD) that enables the CRL4CRBN E3 ligase-dependent ubiquitination and degradation of AR.
100-fold more potent than enzalutamide (ENZ) at inhibiting androgen-stimulated transcription of AR target genes, and 10 to 120-fold more potent than ENZ at inhibiting AR-dependent proliferation of multiple prostate cancer cell lines in vitro.
BMS-986365 demonstrates on-target activity, degrading AR, suppressing AR signaling, and inhibiting tumor growth in animal models of advanced prostate cancer, with tumor volume reductions of 63-92% in therapy resistant patient-derived xenografts, including those with acquired resistance to ENZ.
| M.Wt | 818.92 | |
| Formula | C41H45F3N8O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-((R)-4-(2-(4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-ethylphenoxy)ethyl)-2-methylpiperazin-1-yl)-N-(3-((2,6-dioxopiperidin-3-yl)amino)phenyl)acetamide |
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1. Shuichan Xu, et al. Cancer Res (2024) 84 (7_Supplement): ND02.
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