BI-2536 is a potent and selective inhibitor of PLK1 with IC50 of 0.83 nM.
BI-2536 also weakly inhibits the activities of PLK2 and PLK3 (IC50=3.5 nM and 9.0 nM, respectively), displays >1,000-fold selectivity to a panel of 63 other protein kinases.
BI-2536 causes a mitotic arrest and induces apoptosis in human cancer cell lines, inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens.
BI-2536 also inhibits BRD4 with IC50 of 25 nM.
