199986-75-9
基本信息
CVT-313游離態(tài)
CDK2抑制劑(CVT-313)
NG 26
D6S82E
CVT-313
CS-2441
CVT-313, >98%
CVT-313(NG-26)
CDK2 INHIBITOR III
CVT 313
NG 26
CVT313
NG26
CVT-313 (CDK2 INHIBITOR III)
物理化學(xué)性質(zhì)
常見問題列表
Target | Value |
CDK2
(Cell-free assay) | 0.5 μM |
CVT-313 (Cdk2 Inhibitor III) has been shown to inhibit other kinases, but at much higher IC 50 values, i.e., CDK1 (IC 50 =4.2 μM), CDK4 D1 (IC 50 =215 μM), and MAPK/PKA/PKC (IC 50 >1.25 mM), compared to CDK2 (IC 50 =0.5 μM). CVT-313 has been shown to have profound effects on cell proliferation at concentrations of 5-20 μM. CVT-313 is a potent CDK2 inhibitor, which is identified from a purine analog library with an IC 50 of 0.5 μM in vitro. Inhibition is competitive with respect to ATP (K i =95 nM), and selective CVT-313 has no effect on other, nonrelated ATP-dependent serine/threonine kinases. When added to CDK1 or CDK4, a 8.5- and 430-fold higher concentration of CVT-313 is required for half-maximal inhibition of the enzyme activity. Using normal and tumor human/murine cell lines, the effects of CVT-313 on cell proliferation is measured. The IC 50 for growth inhibition ranged from 1.25 to 20 μM.