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。

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

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].

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].

2417302-07-7

C23H26F3N6OP

490.46

CDK7-IN-3

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