D-64131

74588-78-6

C16H13NO2

DMSO : >= 100 mg/mL (397.96 mM)

Cell Cycle/DNA Damage; Cytoskeleton

D-64131 is a novel inhibitor of Tubulin polymerization that competitively binds with [(3)H]colchicine to alphabeta-Tubulin. IC50 Value: N/A Target: Microtubule/Tubulin in vitro: D-64131 is cytotoxic and inhibits tumor cell proliferation in vitro (IC50 = 74 nM). D-64131 prevents growth of tumor models in mice following oral administration in vivo. D-64131 has significant potential in cancer treatment. The proliferation of tumor cells from 12 of 14 different organs and tissues was inhibited with mean IC(50)s of 62 nM by D-64131. in vivo: In animal studies, no signs of systemic toxicity were observed after p.o. dosages of up to 400 mg/kg of D-64131. In xenograft experiments with the human amelanoic melanoma MEXF 989, D-64131 was highly active with treatment resulting in a growth delay of 23.4 days at 400 mg/kg. Therefore, D-64131 and analogues have the potential to be developed for cancer therapy, replacing or supplementing standard therapy regimens with tubulin-targeting drugs from natural sources.