CGP60474 是一种高效的抗内毒素药物，抑制细胞周期蛋白依赖激酶(CDK) ，抑制CDK1/B、CDK2/E、CDK2/a、CDK4/D、CDK5/p25、CDK7/H 和 CDK9/T 的IC50分别为 26、3、4、216、10、200 和 13 nM。它是选择性和 ATP 竞争性PKC抑制剂。

CGP60474 is an inhibitor of VEGFR-2 (IC50 = 84 nM) and an inhibitor of ATP-competitive PKC. CGP60474 is also a highly potent anti-endotoxemic agent and inhibits cyclin-dependent kinase (CDK) potently.

The IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/CyclinB, CDK2/CyclinE, CDK2/CyclinA, CDK5/p25, CDK7/CyclinH, CDK4/CyclinD and CDK9/cycT, respectively[4].

In the LPS endotoxemia model, CGP60474 (10?mg/kg; i.p.) inhibits the IL-6 level and increases the survival rate[3].

164658-13-3

C18H18ClN5O

355.82

H2O:< 0.1 mg/mL (insoluble)
DMSO:50 mg/mL (140.52 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years