CDK9-IN-7 (compound 21e) 是一种高效选择性的，具有口服活性的 CDK9/cyclin T 抑制剂 (IC50=11 nM)，与抑制其他 CDK 相比更有效 (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM)。CDK9-IN-7 具有抗癌活性并没有明显的毒性。CDK9-IN-7 诱导非小细胞肺癌 (NSCLC) 细胞凋亡，在 G2 期阻滞细胞周期，并具有抑制非小细胞肺癌干度的特性。
CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC[1]. CDK9/cyclinT1|11 nM (IC50)|CDK4/cyclin D|148 nM (IC50)|CDK6/cyclinD|145 nM (IC50)
CDK9-IN-7 displays exceptional potency against NSCLC cell lines, especial A549 and H1299 with IC50 values less than 0.5 µM. In the drug-resistant NSCLC cell line H1975, CDK9-IN-7 also exhibits good inhibition potency with an IC50 value of 0.837 µM[1].
[1]. Wang X, et al. Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer. Eur J Med Chem. 2019 Jul 25;181:111535.
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