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CSRM617 hydrochloride
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。
CSRM617 hydrochloride图片
CAS NO:1353749-74-2
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

产品名称
CSRM617 hydrochloride(787504-88-5 Free base)
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。

产品描述

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]

体外活性

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].

体内活性

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.

Cas No.

1353749-74-2

分子式

C10H14ClN3O5

分子量

291.69

别名

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

储存和溶解度

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