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1209002-43-6

英文名称 VMY 1-103
CAS 1209002-43-6
分子式 C34H42ClN9O4S
分子量 708.27
MOL 文件 1209002-43-6.mol
1209002-43-6 结构式 1209002-43-6 结构式

基本信息

英文别名
VMY 1-103
2-chloro-N-[2-[[5-(dimethylamino)naphthalen-1-yl]sulfonylamino]ethyl]-4-[[2-[[(2R)-1-hydroxy-3-methylbutan-2-yl]amino]-9-propan-2-ylpurin-6-yl]amino]benzamide

物理化学性质

密度1.39±0.1 g/cm3(Predicted)
酸度系数(pKa)10.91±0.50(Predicted)

应用领域

用途一
VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 , but not purvalanol B, significantly decreased the proportion of cells in S phase and increased the proportion of cells in G(2)/M. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death Receptors DR4 and DR5, Bax and Bad while decreasing the number of viable cells, all supporting apoptosis as a mechanism of cell death. VMY-1-103 possesses unique antiproliferative capabilities and that this compound may form the basis of a new candidate drug to treat medulloblastoma.

常见问题列表

概述
VMY-1-103 是细胞周期蛋白/细胞周期蛋白依赖性激酶复合物 (cyclin/Cdk complex) 的抑制剂,可以在 G1 期阻滞细胞周期。VMY-1-103 可降低线粒体膜电位,诱导 p53 磷酸化和 PARP 裂解,激活 caspase-3,从而诱导前列腺癌细胞 LNCaP 凋亡 (apoptosis)。
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