CSRM617 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 通过切割 Caspase-3 和 PARP 诱导细胞凋亡 (apoptosis)。CSRM617 hydrochloride 在小鼠的前列腺癌模型中耐受性良好。

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd 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

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.

CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth in SCID mice with 22Rv1 xenograft.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.

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Apoptosis

Apoptosis

Apoptosis | Androgen Receptor

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1353749-74-2

291.69

C10H14ClN3O5

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (428.54 mM; 超声助溶 )

Cl.NC(CO)C(=O)N\N=C\c1ccc(O)c(O)c1O

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(-20℃)

With Ice Pack

≥ 2 years