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首页-抗体药物偶连体和PROTACs-PROTAC-BMS-986365
BMS-986365

Chemical Structure : BMS-986365

CAS No.: 2446928-30-7

BMS-986365 (CC-94676, BMS986365, CC94676)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 818.92
分子式 C41H45F3N8O5S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

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

参考文献

1. Shuichan Xu, et al. Cancer Res (2024) 84 (7_Supplement): ND02.

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