CSRM617 hydrochloride is a selective small-molecule inhibitor ofthe transcription factor ONECUT2(OC2, a master regulator of androgen receptor) with aK_dof 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride inducesapoptosisby appearance of cleaved Caspase-3 andPARP. CSRM617 hydrochloride is well tolerated in the prostatecancermouse model^[1]

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 results in 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 tumor growth in SCID mice with 22Rv1 xenograft^[1].

291.69

Solid

C₁₀H₁₄ClN₃O₅

1353749-74-2

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)