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MK-5108 (VX-689)
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
阿拉丁 | 生产商 | 上海 | 现货 |
货号 | CAS号 | 操作 |
---|---|---|
M127979-10mg | 1010085-13-8 | 询底价 |
M127979-1mg | 1010085-13-8 | 询底价 |
M127979-50mg | 1010085-13-8 | 询底价 |
M127979-5mg | 1010085-13-8 | 询底价 |
- 分子式 C22H21ClFN3O3S
- 分子量461.94
属性
溶解性 |
|
存贮条件 | 储存温度-20°C |
描述
备注 | MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. Phase 1. |
生化机理 |
MK-5108 (VX-689) is a highly selective Aurora-A kinase inhibitor with an IC50 of 0.064 nM. MK-5108 is a novel small molecule with potent inhibitory activity against Aurora-A kinase. Although most of the Aurora-kinase inhibitors target both Aurora-A and Aurora-B, MK-5108 specifically inhibited Aurora-A kinase in a panel of protein kinase assays. Inhibition of Aurora-A by MK-5108 in cultured cells induced cell cycle arrest at the G2-M phase in flow cytometry analysis. The effect was confirmed by the accumulation of cells with expression of phosphorylated Histone H3 and inhibition of Aurora-A autophosphorylation by immunostaining assays. MK-5108 also induced phosphorylated Histone H3 in skin and xenograft tumor tissues in a nude rat xenograft model. MK-5108 inhibited growth of human tumor cell lines in culture and in different xenograft models. Furthermore, the combination of MK-5108 and docetaxel showed enhanced antitumor activities compared with control and docetaxel alone–treated animals without exacerbating the adverse effects of docetaxel. MK-5108 is currently tested in clinical trials and offers a new therapeutic approach to combat human cancers as a single agent or in combination with existing taxane therapies. |
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途