ELR510444

Description: ELR-510444 is a novel and potent inhibitor of microtubule polymeirzation (also called microtubule disruptor or mitotic inhibitor) with potential antivascular effects and in vivo antitumor efficacy, it can cause a loss of cellular microtubules and the formation of aberrant mitotic spindles which lead to mitotic arrest and apoptosis of cancer cells. ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window. Studies in tumor endothelial cells show that a low concentration of ELR510444 (30 nM) rapidly alters endothelial cell shape, similar to the effect of the vascular disrupting agent combretastatin A4.

References: J Pharmacol Exp Ther. 2011 Mar; 336(3):652-60.