中文名称:

CVT 313

中文同义词:

CDK2抑制剂(CVT-313);CVT-313游离态;化合物CVT313

英文名称:

2(BIS-(HYDROXYETHYL)AMINO)-6-(4-METHOXYBENZYLAMINO)-9-ISOPROPYL-PURINE

英文同义词:

CVT-313;CDK2 INHIBITOR III;2(BIS-(HYDROXYETHYL)AMINO)-6-(4-METHOXYBENZYLAMINO)-9-ISOPROPYL-PURINE;Anti-ABHD16A antibody produced in rabbit;BAT5;D6S82E;2,2-(9-isopropyl-6-(4-methoxybenzylamino)-9H-purin-2-ylazanediyl)diethanol;CVT-313(NG-26)

CAS号:

199986-75-9

分子式:

C20H28N6O3

分子量:

400.47

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

199986-75-9.mol

沸点 

652.3±65.0 °C(Predicted)

密度 

1.30±0.1 g/cm3(Predicted)

储存条件 

Sealed in dry,Store in freezer, under -20°C

酸度系数(pKa)

13.95±0.10(Predicted)

形态

White solid

InChIKey

NQVIIUBWMBHLOZ-UHFFFAOYSA-N

生物活性

CVT-313是有效的CDK2抑制剂，在体外的IC50值为0.5 μM。它对其他非相关的、依赖于ATP的丝氨酸/苏氨酸激酶没有作用。

靶点

Target Value CDK2 (Cell-free assay) 0.5 μM

Target

Value

CDK2 (Cell-free assay)

0.5 μM

体外研究

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.