CAN508 是一种有效的 ATP 竞争性 CDK9/cyclin T1 抑制剂，IC50 为 0.35 μM。它还是 CDK2-cyclin E 对 ATP 的竞争性抑制剂，Ki 和 IC50 值分别为 13.3 和 20 μM。它对 CDK9/cyclin T 的选择性是其他 CDK/cyclin 复合物的 38 倍，有抗肿瘤活性。

CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 μM, respectively.CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.

The most potent inhibitor,CAN508, reduced the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.?Further observed cellular effects included decreased phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibition of mRNA synthesis, and induction of the tumor suppressor protein p53, all of which are consistent with inhibition of CDK9.

140651-18-9

C9H10N6O

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DMSO:250 mg/mL (1145.63 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years