GSK1070916 is a potent, selective and ATP-competitive inhibitor of Aurora B and Aurora C with Ki of 0.38 nM and 1.5 nM, respectively.
GSK1070916 displays >250-fold selectivity over Aurora A; shows potent antiproliferative effect (EC50=7 nM) in A549 human lung cancer cells.
GSK1070916 causes inhibition of histone H3 phosphorylation at serine 10 in human colon cancer (Colo205) and tumor regression in human leukemia (HL-60) in mice.
