N-(5-(5-Cyanothiophen-2-yl)-2-methylphenyl)-4-methylbenzenesulfonamide

BeschreibungELR510444 is an inhibitor of tubulin polymerization (IC50 = 10 μM) that binds to tubulin at the colchicine binding site. It induces microtubule depolymerization in A-10 cells (EC50 = 21 nM). ELR510444 inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest. Oral administration of ELR510444 (3-6 mg/kg) reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner. ELR510444 also inhibits hypoxia-inducible factor 1α (HIF-1α) in RCC4 cells in a concentration-dependent manner.