Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.
IC50&Target
β-tubulin
体外研究
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.
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.
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.
Cell Cycle Analysis
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
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.
体内研究
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.
Animal Model:
Male athymic nude mice (nu/nu) (6-8 week-old, 20-25 g) injected with
CCRF-CEM cells
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.
分子式
C13H7NO3F6S
分子量
371.26
CAS号
195533-53-0
中文名称
巴他布林
运输条件
Room temperature in continental US; may vary elsewhere.