CSRM617 hydrochloride

立即咨询

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1353749-74-2

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议

产品介绍

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K_d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。

生物活性

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]

体外研究
(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^[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].

体内研究
(In Vivo)

CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth 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.

分子量

291.69

性状

Solid

Formula

C₁₀H₁₄ClN₃O₅

CAS 号

1353749-74-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)