CSRM617 hydrochloride 

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a K_d of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model^[1]

CSRM617 (0.01-100 μM；48 小时) 盐酸盐抑制多种 PC 细胞系的细胞生长：PC-3、22RV1、LNCaP、C4-2 细胞^[1]。
CSRM617 (10 -20 μM；48 小时) hydrochloride 诱导 22Rv1 细胞凋亡，导致细胞死亡，呈浓度依赖性^[1]。
CSRM617 (20 μM；72 hours) hydrochloride 诱导细胞凋亡22Rv1 细胞出现裂解的 Caspase-3 和 PARP^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CSRM617 (50 mg/kg；口服；每日一次，持续 20 天) 抑制 22Rv1 异种移植的 SCID 小鼠的肿瘤生长^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

291.69

C₁₀H₁₄ClN₃O₅

1353749-74-2

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Rotinen M, et, al. ONECUT2 is a targetable master regulator of lethal prostate cancer that suppresses the androgen axis. Nat Med. 2018 Dec;24(12):1887-1898.  [Content Brief]