Cevipabulin fumarate

Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [³H]NSC 49842 to tubulin, with an IC₅₀ of 18-40 nM for cytotoxicity in human tumor cell line^[1][2]. IC50 & Target:IC50: 18-40 nM (microtubule in human tumor cells)^[1]. In Vitro:Cevipabulin (0-50 nM, 72 hours) shows good activity (between 18 and 40 nM IC₅₀ values) on cell lines from ovarian, breast, prostate, and cervical tumors^[1].
Flow cytometry experiments reveal that, Cevipabulin (TTI-237) at low concentrations (20-40 nM) produces sub-G₁ nuclei and, at concentrations above 50 nM, it causes a strong G₂-M block^[1]. In Vivo:Cevipabulin (TTI-2370)( 5, 10, 15, and 20 mg/kg, every 4 days for 4 cycles, in mice) is active by i.v. and p.o. administration against human tumor xenografts, showing dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg^[1].