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, directly binds to OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the mouse model of prostate cancer [1]

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

DMSO:45 mg/mL (154.27 mM)

CSRM617 (0.01-100 μM; 48 hours) hydrochloride inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells [1]. CSRM617 (10-20 μM; 48 hours) hydrochloride induces apoptosis in 22Rv1 cells leading to cell death in a concentration-dependent fashion [1]. CSRM617 (20 μM; 72 hours) hydrochloride induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP [1].

CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits the growth of tumor in SCID mice with 22Rv1 xenograft [1]. Animal Model: SCID mice with 22Rv1 xenograft [1] Dosage: 50 mg/kg Administration: Oral administration; daily, for 20 days Result: Elicited a significant reduction in the onset and growth of diffuse metastases.