| 溶解性 | DMSO 92 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| 存贮条件 | 储存温度-20°C |
| 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. |
MK-5108(VX-689),Aurora A抑制剂
MK-5108 (VX-689) （订货以英文为准）
编号：M127979
CAS号：1010085-13-8
分子式：C22H21CLFN3O3S
分子量：461.94
| 产品名称 | MK-5108 (VX-689) |
| 中文名称 | MK-5108(VX-689),Aurora A抑制剂 |
| CAS号 | 1010085-13-8 |
| 分子式（M.F.） | C22H21CLFN3O3S |
| 分子量（M.W.） | 461.94 |
| 储存条件 | -20°C储存 |
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