CSRM617 hydrochloride 是转录因子ONECUT2(OC2，雄激素受体 AR 的主要调节剂) 的选择性小分子抑制剂，在 SPR 测定中Kd为 7.43 uM，直接与 OC2-HOX 结构域结合。CSRM617 hydrochloride 通过裂解 Caspase-3 和 PARP 诱导细胞Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。CSRM617 hydrochloride 在小鼠的前列腺癌模型中具有良好的耐受性。

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]

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.

1353749-74-2

C10H14ClN3O5

291.69

CSRM617 hydrochloride(787504-88-5 Free base);CSRM617 hydrochloride

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years