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CYT997 is an inhibitor of microtubule polymerization (IC50 = ~3 µM).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 µM). CYT997 increases human umbilical vein endothelial cell (HUVEC) monolayer permeability (IC50 = ~0.08 µM), 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
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1. CYT997: A novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Mol. Cancer Ther. 8(11), 3036-3045 (2009).
2. The microtubule depolymerizing agent CYT997 causes extensive ablation of tumor vasculature in vivo. J. Pharmacol. Exp. Ther. 339(3), 799-806 (2011).