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 In Vitro CSRM617 (0.01-100 μM; 48 hours) hydrochloride inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells. CSRM617 (10-20 μM; 48 hours) hydrochloride induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion. CSRM617 (20 μM; 72 hours) hydrochloride induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth in SCID mice with 22Rv1 xenograft . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice with 22Rv1 xenograft Dosage: 50 mg/kg Administration: Oral administration; daily, for 20 days Result: Elicited a significant reduction in the onset and growth of diffuse metastases. Form:Solid

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