Unii-T4np8G3K6q

生物活性靶点体外研究体内研究 Unii-T4np8G3K6q 试剂级价格

Unii-T4np8G3K6q

CAS号:195533-53-0
英文名:Unii-T4np8G3K6q
中文名:Unii-T4np8G3K6q
CBNumber:CB82494683
分子式:C13H7F6NO3S
分子量:371.26
MOL File:195533-53-0.mol

Unii-T4np8G3K6q化学性质

沸点 :403.3±55.0 °C(Predicted)
密度 :1.629±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: 100 mg/mL (269.35 mM)
形态 :Solid
酸度系数(pKa) :5.74±0.10(Predicted)
颜色 :White to off-white

Unii-T4np8G3K6q性质、用途与生产工艺

生物活性 Batabulin (T138067) 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 (microtubule) 聚合。Batabulin 影响细胞形态并导致细胞周期停滞，最终诱导凋亡性细胞死亡。
靶点

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.