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SY-5609
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。
SY-5609图片
CAS NO:2417302-07-7
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
CDK7-IN-3
产品介绍
SY-5609 是一种选择性的非共价 CDK7 抑制剂(KD = 0.065 nM),具有抗肿瘤活性并抑制细胞凋亡。

产品描述

SY-5609 is a selective and noncovalent inhibitor of CDK7(KD = 0.065 nM) with antitumor activity and inhibits apoptosis.

体外活性

SY-5609 (126.4 pM-4 μM) has an EC50 of 5.6 nM in the HCC70 cell line[1]. SY-5609 (0.01-10000 nM) exhibits strong antiproliferative effects with IC50s of 1-6 nM in triple-negative breast cancer and ovarian cancer cells including HCC70, MDA-MB453, COV504, A2780, OVCAR3, CAOV3 cells. SY-5609 (100-500 nM) induces apoptosis in HCC70, MDA-MB-468, CAOV3, and OVCAR3 cells. In HCC70 cells, SY-5609 (100-500 nM) induces G2/M cell cycle arrest. SY-5609 (25-500 nM) inhibits the phosphorylation of CDK2 at Thr160 via loss of CAK function[2].

体内活性

In Balb/c nude female mice with HCC70 cell lines, SY-5609 (2 mg/kg/day; orally) induces tumor regression with a plasma exposure of 261.28 ng h/mL, a Cmax of 50.67 ng/mL and an elimination half-life of 3.33 h[2].

Cas No.

2417302-07-7

分子式

C23H26F3N6OP

分子量

490.46

别名

CDK7-IN-3

储存和溶解度

DMSO:36mg/mL (73.4mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years