MK-5108 (VX-689) is a potent, highly selective Aurora-A kinase inhibitor with IC50 of 0.064 nM, displays robust selectivity against Aurora-B (220-fold) and Aurora-C (190-fold) in the biochemical assays.
MK-5108 (VX-689) also exhibits high selectivity for Aurora-A over a panel of 233 kinases, only one kinase (TrkA) with <100-fold selectivity.
MK-5108 (VX-689) inhibits the growth of multiple human cancer cell lines in vitro and in human cancer xenograft models.
MK-5108 (VX-689) MK-5108 significantly enhanced the efficacy of docetaxel without increasing its toxicity.
