ON-01910 is a potent, non-ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC50 = 9 nM), a serine/threonine protein kinase involved in the regulation of cell cycling. It induces apoptosis in a wide array of tumor cell lines (GI50 = 50-200 nM) and blocks the growth of multidrug resistant cancer cell lines. ON-01910 is active in vivo when administered intraperitoneally and synergizes with chemotherapeutic agents, preventing tumor growth or abolishing tumors in human xenograft nude mouse models.
