GSK461364 is a potent, selective, and reversible ATP-competitive PLK1 inhibitor with Ki of 2.2 nM.
GSK461364 displays >390-fold greater selectivity for Plk1 than for Plk2 and Plk3 and 1,000-fold greater selectivity than for a panel of 48 other kinases.
GSK461364 shows antiproliferative activity against >120 tumor cell lines and potently inhibits the proliferation with IC50s of <100 nM.
GSK461364 shows clear antitumor activity in human tumor xenograft models.
