| 应用 |
A selective inhibitor of cell cycle and transcriptional cyclin dependent kinases including Cdk1, Cdk2, and Cdk4. |
| 产品介绍 |
R547是一种有效的，ATP竞争性CDK1/2/4抑制剂，Ki为2 nM/3 nM/1 nM，对CDK7和GSK3α/β作用效果稍弱，而抑制其他激酶活性。Phase 1。 |
| 备注 |
R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. |
| 生化机理 |
R547 is a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases including Cdk1/cyclin B, Cdk2/cyclin E, and Cdk4/cyclin D1. R547 has shown antitumor activity, and may be promising for development of a potential treatment for solid tumors. The cyclin-dependent protein kinases are key regulators of cell cycle progression; altering the expression or activity of Cdk complexes can lead to aberrant cell cycle control, leading to unrestricted cell proliferation. CDK inhibitors have the potential to induce cell cycle arrest and apoptosis in cancer cells, and identifying small-molecule CDK inhibitors has been a major focus in cancer research. |
| 别名 |
[4-氨基-2-[(1-甲磺酰基哌啶-4-基)氨基]嘧啶-5-基](2,3-二氟-6-甲氧基苯基)甲酮;R 547;R-547;[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone |
