MK-5108
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CAS No. | 1010085-13-8 | Cat. No. | BCP04741 |
Name | MK-5108 | ||
Synonyms | MK 5108;VX-689;VX 689;MK5108;VX689; | ||
SMILES | O=C([C@@]1(CC2=NC(NC3=NC=CS3)=CC=C2)CC[C@H](OC4=CC=CC(Cl)=C4F)CC1)O | ||
Chemical Name | |||
Formula | C22H21ClFN3O3S | M. Wt | 461.94 |
Purity | 98% | Storage | Store at 4-8°C |
Description | 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. |
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