Biological Activity |
Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the beta-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death[1]. IC50 & Target: beta-tubulin[1] In Vitro: Batabulin (T138067; 30-300 nM; 24 hours; MCF7 cells) treatment shows approximately 25-30% tetraploid (4n) DNA content in cells, indicating an arrest at the G2/M cell-cycle boundary[1]. Batabulin (T138067; 30-300 nM; 24-48 hours; MCF7 cells) treatment shows 25-30% apoptosis. After a 48-hr exposure to 100 nM Batabulin, approximately 50-80% of the cell population is undergoing apoptosis[1]. Batabulin (T138067) binds covalently and selectively to a subset of the beta-tubulin isotypes, thereby disrupting microtubule polymerization. Covalent modification occurs at a conserved Cys-239 shared by the beta1, beta2, and beta4 tubulin isotypes. Cells exposed to Batabulin become altered in shape, indicating a collapse of the cytoskeleton, and show an increase in chromosomal ploidy[1]. In Vivo: Batabulin (T138067; 40 mg/kg; intraperitoneal injection; once per week; on days 5, 12, and 19; male athymic nude mice) treatment impairs the growth of the drug-sensitive CCRF-CEM tumors[1]. |