Batabulin sodium (T138067 sodium) is an antitumor agent, which covalently and selectively modifies the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin sodium affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death [1].

Batabulin (T138067; 30-300 nM; 24 hours; MCF7 cells) treatment exhibits approximately 25-30% tetraploid (4n) DNA content in cells, suggesting 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 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, indicating a collapse of the cytoskeleton, and show an increase in chromosomal ploidy [1]. Cell Cycle Analysis [1] Cell Line: MCF7 cells Concentration: 30 nM, 100 nM and 300 nM Incubation Time: 24 hours Result: Showed an arrest at the G2/M cell-cycle boundary. Apoptosis Analysis [1] Cell Line: MCF7 cells Concentration: 30 nM, 100 nM and 300 nM Incubation Time: 24 hours or 48 hours Result: 25-30% of cells showed the reduced DNA content characteristic of apoptotic cells.

Batabulin (T138067; 40 mg/kg; intraperitoneal injection; once per week; on days 5, 12, and 19; male athymic nude mice) treatment impairs the drug-sensitive CCRF-CEM tumors growth [1]. Animal Model: Male athymic nude mice ( nu/nu ) (6-8 week-old, 20-25 g) injected with CCRF-CEM cells [1] Dosage: 40 mg/kg Administration: Intraperitoneal injection; once per week; on days 5, 12, and 19 Result: Impaired the growth of the drug-sensitive CCRF-CEM tumors.