PURVALANOL A

生物活性体外研究生物活性靶点体外研究 PURVALANOL A 试剂级价格

PURVALANOL A

CAS号:212844-53-6
英文名:PURVALANOL A
中文名:PURVALANOL A
CBNumber:CB5283664
分子式:C19H25ClN6O
分子量:388.89
MOL File:212844-53-6.mol

PURVALANOL A化学性质

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
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

安全信息

WGK Germany :3
海关编码 :2933599590

PURVALANOL A性质、用途与生产工艺

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
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。