Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis.In Vitro:Tubulin inhibitor 11 (Compound 48; 0.03-0.1 μM; 12 hours) causes cell cycle arrest at G2/M phase. Tubulin inhibitor 11 reduces cdc2 phosphorylation and increases cyclin B1 and phosphorylation of histone H3 at Ser10 in cells.
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM; 48 hours) causes cancer cell apoptosis.
Tubulin inhibitor 11 (Compound 48) demonstrates favorable antiproliferative activities in DU145 cells with an IC50 of 8 nM.
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM) significantly reduces the expression levels of acetyl-α-tubulin and α-tubulin in a dose-dependent manner.
In Vivo:Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies.