D-64131

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM. [1]

The polymerization of bovine brain tubulin as well as binding of [3H] colchicine to biotinylated αβ-tubulin was dose-dependently inhibited by D-64131. Many cancer cells display abnormal microtubule structures, such as fragmented mitotic spindles or multiple spindle poles after treatment with D-64131. Nuclear blebbing and abnormal nuclear structures typical for apoptotic cells are detectable in many cells treated with D-64131. In nude mice, D-64131 proved to be well tolerated and highly active against the human amelanoic melanoma MEXF 989 tumor xenograft. D-64131 treatment resulted in significant tumor growth inhibition during treatment. [1]

Reference:
1. Beckers T, Reissmann T, Schmidt M et al.  2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors. Cancer Res. 2002 Jun 1;62(11):3113-9.