CAY10574 是一种有效的 ATP 竞争性 CDK9/cyclin T1 抑制剂，IC50 为 0.35 μM。 CAY10574 对 CDK9/cyclin T 的选择性是其他 CDK/cyclin 复合物的 38 倍。抗肿瘤活性。
| Cas No. | 140651-18-9 |
| Canonical SMILES | Oc1ccc(cc1)\N=N/c1c(N)n[nH]c1N |
| 分子式 | C9H10N6O |
| 分子量 | 218.2 |
| 溶解度 | DMF: 0.5 mg/ml,DMSO: 0.5 mg/ml |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. CAY10574 is a potent, selective inhibitor of Cdk9 in vitro with an IC50 value 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. CAY10574 reduces the population of S-phase cells of the cancer cell line HT-29 and blocks proliferation of several other cancer cell lines including MCF-7, HOS, G361, and K562 cells with IC50 values of 33, 49, 64, and 62 µM, respectively. |
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