CYT997 is an inhibitor of microtubule polymerization (IC50 = ~3 ?M).1 It induces cell cycle arrest at the G2/M phase and is cytotoxic against a panel of cancer cell lines (IC50s = 0.009-0.101 ?M). CYT997 increases human umbilical vein endothelial cell (HUVEC) monolayer permeability (IC50 = ~0.08 ?M), a marker of vascular collapse. It decreases liver metastasis in a murine DMH-induced colon cancer model when administered at doses of 5, 10, and 15 mg/kg.2
1.Burns, C.J., Fantino, E., Philips, I.D., et al.CYT997: A novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivoMol. Cancer Ther.8(11)3036-3045(2009) 2.Burns, C.J., Fantino, E., Powell, A.K., et al.The microtubule depolymerizing agent CYT997 causes extensive ablation of tumor vasculature in vivoJ. Pharmacol. Exp. Ther.339(3)799-806(2011)