Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively. It exhibits greater than 20-fold selectivity for Plk1 over FAK, MLCK, and the tyrosine protein kinase Fes, and has minimal activity against a panel of 282 other kinases. It inhibits the proliferation of various cancer cell lines, including MDR1-expressing tumors, and also prevents tumor growth in several human cancer cell xenograft models, including a disseminated model of AML- and MDR1-expressing hematological tumors.
