Description
Rigosertib sodium (ON 01910.Na) is a potent, non-ATP-competitive PLK1 inhibitor (IC50=9-10nM), selectively induces mitotic G2/M arrest and apoptosis in cancer cells; also exhibits inhibitory activity against PDGFR, Abl, and Flt-1, at higher concentrations, inhibits CDK1, Plk2, Src, and Fyn; demonstrates in vitro cytotoxicity against DU145 and K562 cells with IC50 of 100 and 15nM; potently inhibits tumor growth in a variety of xenograft nude mouse models, does not exhibit hematotoxicity, liver damage, or neurotoxicity shows strong synergy with several chemotherapeutic agents. Blood Cancer Phase 3 Clinical