Description
An inhibitor of the Plk1 polo-box domain (apparent IC50 = 4.8 µM); selective for the Plk1 PBD over Plk2 and Plk3 PBDs (IC50s = 18.7 and 53.9 µM, respectively); induces cell cycle arrest at the G2/M phase, apoptosis, and mislocalization of Plk1 in HeLa cells at 5, 10, and 25 µM; reduces cell proliferation in a panel of 10 cancer cell lines (EC50s = 15-35 µM); reduces tumor growth and induces intratumor apoptosis in an MDA-MB-231 mouse xenograft model at 40 mg/kg