Batabulin 是一种抗肿瘤剂,可与 β-微管蛋白同种型的子集共价且选择性地结合,从而破坏微管聚合。它影响细胞形态并导致细胞周期停滞,最终诱导细胞凋亡。
产品描述
Batabulin is an antitumor compound, 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 induce apoptotic cell death.
体外活性
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.
体内活性
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.
Cas No.
195533-53-0
分子式
C13H7F6NO3S
分子量
371.26
别名
T138067;巴他布林
储存和溶解度
DMSO:100 mg/mL (269.35 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years