MK-5108, also known as VX689, is a novel small molecule with potent inhibitory activity against Aurora-A kinase. MK-5108 specifically inhibited Aurora-A kinase in a panel of protein kinase 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. 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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