195533-53-0
基本信息
T 138067
Batabulin
Batabulin [inn]
Unii-T4np8G3K6q
2,3,4,5,6-pentafluoro-N-(3-fluoro-4-methoxyphenyl)benzenesulfonamide
N-(3-Fluoro-4-methoxyphenyl)-2,3,4,5,6-pentafluorobenzenesulfonamide
Benzenesulfonamide, 2,3,4,5,6-pentafluoro-N-(3-fluoro-4-methoxyphenyl)-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
β-tubulin
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. |
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. |