CVT-313
产品说明书
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同义名 : | Cdk2 Inhibitor III; Cyclin-dependent kinase 2 Inhibitor III |
| CAS号 : | 199986-75-9 | |
| 货号 : | A421689 | |
| 分子式 : | C20H28N6O3 | |
| 纯度 : | 98% | |
| 分子量 : | 400.47 | |
| MDL号 : | MFCD06411412 | |
| 存储条件： |
Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Cell cycle progression in mammalian cells is regulated by a family of cyclin-dependent protein kinases (CDKs). CDK2 is a serine/threonine kinase whose activity is essential for the G1 to S transition during cell division. CVT-313 is a potent, selective and ATP-competitive CDK2 inhibitor with an IC50 of 0.5 μM and a Ki of 95 nM, and has no effect on other, nonrelated ATP-dependent serine/threonine kinases. The growth of mouse, rat, and human cells in culture was inhibited by CVT-313 with the IC50 for growth arrest ranging from 1.25 to 20 μM. When nonsynchronized MRC-5 cells were treated with CVT-313 (6.25 μM) for 36 h, most of these cells had a 2 N DNA content, consistent with a G1/S arrest. After removal of CVT313, cells reentered the cell cycle suggesting that the inhibition of cell proliferation was reversible. Moreover, if CVT-313 (6.25 mM) was added at 0, 4, or 8 h after serum stimulation, Rb hyperphosphorylation was inhibited. A brief intraluminal exposure of CVT-313 (1.25 mg/kg for 15 min) to a denuded rat carotid artery resulted in more than 80% inhibition of neointima formation[3]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.50mL 0.50mL 0.25mL |
12.49mL 2.50mL 1.25mL |
24.97mL 4.99mL 2.50mL |
| 参考文献 |
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