2446928-30-7
Chemical Structure
BMS-986365
Synonym(s): CC-94676
- CAS No.: 2446928-30-7
- Formula:C41H45F3N8O5S
- Molecular Weight:818.91
InChIKey: YUVGVJYLOFTILT-NHYGQJMQSA-N
SMILES: N#CC1=C(C(F)(F)F)C=C(N2C(N(C3=CC=C(OCCN4C[C@@H](C)N(CC(NC5=CC=CC(NC6C(NC(CC6)=O)=O)=C5)=O)CC4)C(CC)=C3)C(C)(C)C2=O)=S)C=C1
Biological Activity: BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC)[1][2][3][4].
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BMS-986365 | 99.92% | BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC). | ||||||||||||||||||||
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- [1]. Xu S, 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[J]. Cancer Research, 2024, 84(7_Supplement): ND02-ND02.
- [2]. Rathkopf DE, et al. Safety and clinical activity of BMS-986365 (CC-94676), a dual androgen receptor ligand-directed degrader and antagonist, in heavily pretreated patients with metastatic castration-resistant prostate cancer. Ann Oncol. 2024 Sep 16:S0923-7534(24)04001-8. [Content Brief]
- [3]. Nayak S, et al. Discovery of BMS-986365, a first-in-class dual androgen receptor ligand-directed degrader (AR LDD) and antagonist, for the treatment of advanced prostate cancer. Clin Cancer Res. 2025 Aug 11. [Content Brief]
- [4]. Rathkopf D E, et al. First-in-human phase 1 study of CC-94676, a first-in-class androgen receptor (AR) ligand-directed degrader (LDD), in patients (pts) with metastatic castration-resistant prostate cancer (mCRPC)[J]. 2024.
Keywords
