Cevipabulin is an activator of microtubule polymerization.1,2 It induces aggregation of isolated bovine brain tubulin in a concentration-dependent manner.1 Cevipabulin (100 ?M) inhibits binding of vinblastine , but not colchicine , to tubulin in cell-free assays. It induces mitotic block in HeLa cells when used at a concentration of 68 nM and is cytotoxic to MDA-MB-468, MDA-MB-435, LNCaP, SKOV3, and HeLa cancer cell lines (IC50s = 18-40 nM). Cevipabulin (20 mg/kg, i.v.) reduces tumor growth in a LoVo colon adenocarcinoma mouse xenograft model.
1.Beyer, C.F., Zhang, N., Hernandez, R., et al.TTI-237: A novel microtubule-active compound with in vivo antitumor activityCancer Res.68(7)2292-2300(2008) 2.Beyer, C.F., Zhang, N., Hernandez, R., et al.The microtubule-active antitumor compound TTI-237 has both paclitaxel-like and vincristine-like propertiesCancer Chemother. Pharmacol.64(4)681-689(2009)