BMS-986365

• CAT Number: I047738
• CAS Number: 2446928-30-7
• Molecular Formula: C41H45F3N8O5S
• Molecular Weight: 818.91
• Purity: ≥95%
• IUPAC Name: 2-[(2R)-4-[2-[4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-ethylphenoxy]ethyl]-2-methylpiperazin-1-yl]-N-[3-[(2,6-dioxopiperidin-3-yl)amino]phenyl]acetamide
• InChI: InChI=1S/C41H45F3N8O5S/c1-5-26-19-31(52-39(58)51(38(56)40(52,3)4)30-10-9-27(22-45)32(21-30)41(42,43)44)11-13-34(26)57-18-17-49-15-16-50(25(2)23-49)24-36(54)47-29-8-6-7-28(20-29)46-33-12-14-35(53)48-37(33)55/h6-11,13,19-21,25,33,46H,5,12,14-18,23-24H2,1-4H3,(H,47,54)(H,48,53,55)/t25-,33?/m1/s1
• SMILES: CCC1=C(C=CC(=C1)N2C(=S)N(C(=O)C2(C)C)C3=CC(=C(C=C3)C#N)C(F)(F)F)OCCN4CCN([C@@H](C4)C)CC(=O)NC5=CC=CC(=C5)NC6CCC(=O)NC6=O

BMS-986365 is a highly potent and selective androgen receptor (AR) degrader that induces rapid and deep degradation of both wildtype and mutant forms of the receptor residing in either the cytoplasmic or nuclear compartments of the cell. Moreover, BMS-986365 is a ligand-directed degrader (LDD) that enables the CRL4CRBN E3 ligase-dependent ubiquitination and degradation of AR (DC50 10 to 40 nM, Ymin 7 to 19%). KEYWORDS: BMS-986365 | Supplier | AR degrader | CC-94676 | BMS986365 | BMS 986365 | CC94676 | CC 94676 | CAS [2446928-30-7] | Androgenic hormones | Androgen (AR) | Degrader | Receptors | Advanced prostate cancer

Reference

S Xu et al. Abstract ND02: Discovery of BMS-986365, a ligand-directed androgen receptor degrader (AR LDD) with a dual mechanism-of-action and best-in-class potential, for the treatment of advanced prostate cancer. Cancer Res. 2024 Apr 1;84(7):ND02.