PURVALANOL A
中文名称:
PURVALANOL A
中文同义词:
CDK抑制剂(PURVALANOL A);(R)-2-((6-((3-氯苯基)氨基)-9-异丙基-9H-嘌呤-2-基)氨基)-3-甲基丁-1-醇;PURVALANOL A 抑制剂
英文名称:
PURVALANOL A
英文同义词:
PURVALANOL A;NG-60;6-(3-CHLOROANILINO)-2(1R)-ISOPROPYL-2-HYDROXYETHYLAMINO-9-ISOPROPYLPURINE;(2R)-2-[[6-[(3-CHLOROPHENYL)AMINO]-9-(1-METHYLETHYL)-9H-PURIN-2-YL]AMINO]-3-METHYL-1-BUTANOL;2-(1R-ISOPROPOYL-2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYLPURINE;2-(1R-ISOPROPYL-2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYL-PURINE;CH61386;2R)-2-[[6-[(3-Chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanolCDKinhibitor.
CAS号:
212844-53-6
分子式:
C19H25ClN6O
分子量:
388.89
EINECS号:
相关类别:
小分子抑制剂，天然产物;抑制剂;小分子抑制剂;细胞生物学试剂;Inhibitors;Signalling
Mol文件:
212844-53-6.mol
沸点
590.5±60.0 °C(Predicted)
密度
1.33±0.1 g/cm3(Predicted)
储存条件
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度
methylene chloride: 50 mg/mL, clear, colorless
形态
powder
酸度系数(pKa)
14.51±0.10(Predicted)
颜色
off-white
生物活性
Purvalanol A 是一种有效的，细胞渗透性 CDK 抑制剂，对cdc2-cyclin B，cdk2-cyclin A，cdk2-cyclin E，和 cdk4-cyclin D1的 IC50 分别为 4 nM，70 nM，35 nM，和 850 nM。
体外研究
Purvalanol A decreases cell viability in dose-dependent manner in MCF-7 and MDA-MB-231 cell lines. Purvalanol A induces cell viability loss by 50 % in MCF-7 cells but MDA-MB-231 cells sre less sensitive to Purvalanol A (32 % decreases in cell viability). Purvalanol A induces mitochondria-mediated apoptosis in MCF-7 and MDA-MB-231 cells. Purvalanol A effectively prevents c-Src-mediated transformation by inhibiting both cell cycle progression and c-Src signaling, and effectively suppresses the anchorage independent growth of some human cancer cells in which c-Src is up-regulated. Purvalanol A has a stronger inhibitory effect on the anchorage-independent growth of HT29 and SW480 human colon cancer cells.
生物活性
Purvalanol A 是一种有效的，细胞渗透性 CDK 抑制剂，对cdc2-cyclin B，cdk2-cyclin A，cdk2-cyclin E，和 cdk4-cyclin D1的 IC50 分别为 4 nM，70 nM，35 nM，和 850 nM。Purvalanol A 可诱导内质网应激介导的凋亡与自噬。
靶点
Target Value
Cdc2/CyclinB
() 4 nM
CDK2/CyclinE 35 nM
CDK2/CyclinA 70 nM
CDK4/CyclinD1 850 nM
Target
Value
Cdc2/CyclinB
()
4 nM
CDK2/CyclinE
35 nM
CDK2/CyclinA
70 nM
CDK4/CyclinD1
850 nM
体外研究
Purvalanol A剂量依赖性降低MCF-7和MDA-MB-231细胞系中细胞活性。Purvalanol A在MCF-7细胞中诱导50%的细胞活性损失，而MDA-MB-231细胞对Purvalanol A敏感性较低(细胞活性减少32 %)。Purvalanol A在MCF-7和MDA-MB-231细胞中诱导线粒体介导的细胞凋亡。 Purvalanol A通过抑制细胞周期进程和c-Src信号通路，有效防止c-Src介导转化，并有效抑制一些c-Src上调的人类癌细胞贴壁不依赖性生长。 Purvalanol A对HT29和SW480人结肠癌细胞的贴壁依赖性生长具有强烈的抑制作用。
WGK Germany
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