Cevipabulin is a potent microtubule-active antitumor agent with an IC50 value of 34 nM for cytotoxicity. Cevipabulin inhibits binding of vinblastine at the Vinca alkaloid site of the αβ-tubulin heterodimer. Moreover, Cevipabulin enhances the aggregation of microtubule protein at substoichiometric concentrations and also induces aggregation of highly purified tubulin in the absence of GTP. At low concentrations with cells, Cevipabulin induces mitotic spindle perturbations that do not cause mitotic block but lead to the production of multinuclear G1 cells. Cevipabulin shows good antitumor activity in nude mouse xenograft models of human cancer.

KEYWORDS: Cevipabulin | Microtubule-active agent | TTI-237 | TTI237 | TTI 237 | CAS [849550-05-6] | [925902-82-5] | Cytoskeleton | Tubulin | Inhibitor | Proteins