中文名称:

3-[[4-[2-[(3-氯苯基)氨基]-4-嘧啶基]-2-吡啶基]氨基]-1-丙醇

中文同义词:

3-[[4-[2-[(3-氯苯基)氨基]-4-嘧啶基]-2-吡啶基]氨基]-1-丙醇;PKC抑制剂(CGP60474);3-((4-(2-((3-氯苯基)氨基)嘧啶-4-基)吡啶-2-基)氨基)丙-1-醇

英文名称:

3-[[4-[2-[(3-Chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol

英文同义词:

3-[[4-[2-[(3-Chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-1-propanol;CGP 60474;CS-506;3-[[4-[2-(3-chloroanilino)pyrimidin-4-yl]pyridin-2-yl]amino]propan-1-ol;CGP-60474;CGP 60474;1-Propanol, 3-[[4-[2-[(3-chlorophenyl)amino]-4-pyrimidinyl]-2-pyridinyl]amino]-

CAS号:

164658-13-3

分子式:

C18H18ClN5O

分子量:

355.82

EINECS号:

200-258-5

相关类别:

细胞生物学试剂;细胞周期

Mol文件:

164658-13-3.mol

熔点 

144-147℃

沸点 

630.6±65.0 °C(Predicted)

密度 

1.356

储存条件 

Keep in dark place,Sealed in dry,2-8°C

酸度系数(pKa)

14.93±0.10(Predicted)

生物活性

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

靶点

CDK1-Cyclin B 26 nM (IC 50 ) CDK2/cyclinE 3 nM (IC 50 ) cdk2/cyclin A 4 nM (IC 50 ) CDK4/cyclin D 216 nM (IC 50 ) Cdk5/p25 10 nM (IC 50 ) CDK7/cyclin H 200 nM (IC 50 ) CDK9/cycT 13 nM (IC 50 ) PKC

CDK1-Cyclin B 26 nM (IC 50 )

CDK2/cyclinE 3 nM (IC 50 )

体外研究

CGP60474 (Compound A) is a potent VEGFR-2 inhibitor, with an IC 50 of 84 nM. CGP60474 is also a PKC inhibitor, with competitive kinetics relative to ATP.

体内研究

CGP-60474 (10 mg/kg; i.p.) inhibits the IL-6 level and increases the survival rate in the LPS endotoxemia model. Animal Model: C57Bl/6 mice (LPS endotoxemia model) Dosage: 10 mg/kg Administration: I.p. Result: Had a higher survival rate.

Animal Model:

C57Bl/6 mice (LPS endotoxemia model)

Dosage:

10 mg/kg

Administration:

I.p.

Result:

Had a higher survival rate.