产品描述:
GSK1070916 is a potent and ATP-competitive inhibitor of Aurora kinases B and C (Kis = 0.38 and 1.5 nM, respectively).{43055} It is >250-fold selective for Aurora B and C over Aurora A. GSK1070916 inhibits proliferation of A549 lung cancer cells in vitro (EC50 = 7 nM). It also inhibits proliferation in a panel of 100 tumor cell lines (EC50s = via induction of polyploidy and apoptosis.{43056} In vivo, GSK1070916 inhibits histone H3 phosphorylation in a COLO 205 mouse xenograft model and induces tumor regression in an HL-60 mouse xenograft model.{43055} It also reduces tumor growth in 10 mouse xenograft models, including models of breast, colon, and lung carcinomas as well as leukemias.{43056}