Y06137 是一种有效的特异性 BET 抑制剂，对 BRD4(1) 溴结构域的 Kd 为 81 nM。 Y06137可用于去势抵抗性前列腺癌治疗的研究。

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

Treatment of AR-positive prostate cancer cell lines 22Rv1 cells with Y06137 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels. Y06137 (0.001-100 nM) exhibits low micromolar or nanomolar potencies in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 0.47, 0.84, 0.70, 0.29 μM, respectively[1].

Y06137 (50 mg/kg, i.p.,100 μL) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06137 exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 51%[1].

2226534-49-0

C27H32N4O2

444.57

DMSO:60 mg/mL (134.96 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years