BMS-986365

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].

Product Specifications

CAS Number

[2446928-30-7]

Product Name Alternative

CC-94676

UNSPSC

12352005

Target

Androgen Receptor; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bms-986365.html

Purity

99.92

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C41H45F3N8O5S

Molecular Weight

818.91

References & Citations

[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.|[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.|[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.