A-259745

A-259745 is an orally active antimitotic agent that binds to the colchicine site on tubulin. It exhibits potent in vitro cytotoxic activity against both multidrug-resistant and non-multidrug-resistant cancer cell lines, with ED50 values of 0.018 μM for HCT-15 and 0.028 μM for NCI-H460 cells. A-259745 inhibits tubulin polymerization, disrupting the dynamic equilibrium of the mitotic spindle, causing dividing cells to arrest in the metaphase-anaphase transition, which subsequently induces apoptosis (apoptosis) . In mouse tumor models, A-259745 demonstrates dose-dependent antitumor efficacy and is useful for cancer research.