MK-5108
| CAS号 | 1010085-13-8 | 货号 | BCP04741 |
| 中文名 | MK-5108 | ||
| 英文名 | MK-5108 | ||
| 中文别名 | |||
| 英文别名 | MK 5108;VX-689;VX 689;MK5108;VX689; | ||
| 分子式 | C22H21ClFN3O3S | 分子量 | 461.94 |
| 生物活性 | MK-5108 inhibits Aurora-A activity in an ATP-competitive manner. MK-5108 shows robust selectivity against the other family kinases Aurora-B (220-fold) and Aurora-C (190-fold) in the biochemical assay. MK-5108 also reveals high selectivity for Aurora-A over other protein kinases. MK-5108 inhibits only one kinase (TrkA) with <100-fold selectivity. MK-5108 may be more Aurora-A selective than MLN8054. Consistent with the induction of pHH3-positive cells, MK-5108 induces accumulation of cells in the G2-M phase. MK-5108 inhibits the proliferation of tumor cells including HCC1143, AU565, MCF-7, HCC1806 and CAL85-1 with an IC50 of 0.42 μM, 0.45 μM, 0.52 μM, 0.56μM and 0.74 μM, respectively. MK-5108 decreases cell viability in a dose-dependent fashion in all three cell lines including LEIO285, LEIO505 and SK-LSM1 cells with an IC50 of approximately 100 nM. Incubation with MK-5108 in LEIO285 increases the proportion of cells in G2/M at 48 and 72 hours post-treatment. | ||
| 信号通路 | Cell Cycle/DNA Damage Epigenetics | ||
| 靶 点 | Aurora | ||
结构式
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