Batabulin (T138067) is an antitumor compound that binds covalently and selectively to a subset of the β-tubulin isotypes, disrupting microtubule polymerization. This disruption affects cell morphology, induces cell-cycle arrest, and ultimately leads to apoptotic cell death.

In MCF7 cells, the treatment of Batabulin (T138067; 30-300 nM; 24 hours) shows approximately 25-30% tetraploid (4n) DNA content in cells and 25-30% apoptosis. After a 48-hr exposure to 100 nM Batabulin, approximately 50-80% of the cell population is undergoing apoptosis. Batabulin binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Covalent modification occurs at a conserved Cys-239 shared by the β1, β2, and β4 tubulin isotypes. Cells exposed to Batabulin become altered in shape.

Batabulin (40 mg/kg; i.p.; once per week; on days 5, 12, and 19; male athymic nude mice) treatment impairs the growth of the drug-sensitive CCRF-CEM tumors.