Batabulin-sodium-T138067-sodium-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBatabulin sodiumCat. No.: HY-13563ACAS No.: 195533-98-3Synonyms: T138067 sodium分式: CHFNNaOS分量: 393.24作靶點: Microtubule/Tubulin; Apoptosis作通路: Cell Cycle/DNA Damage; Cytoskeleton; Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solv

2、ent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (317.87 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5430 mL 12.7149 mL 25.4298 mL5 mM 0.5086 mL 2.5430 mL 5.0860 mL10 mM 0.2543 mL 1.2715 mL 2.5430 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活

3、性 Batabulin sodium (T138067 sodium)種抗腫瘤劑，可與 -微管蛋同種型的集共價且選擇性地結(jié)合，從破壞微管 (microtubule) 聚合。Batabulin sodium響細胞形態(tài)并導(dǎo)致細胞周 期停滯，最終誘導(dǎo)凋亡性細胞死亡。IC50 & Target -tubulin 11/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Batabulin (T138067; 30-300 nM; 24 hours; MCF7 cells) treatment shows approximately 25-30% te

4、traploid(4n) DNA content in cells, indicating 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-hrexposure to 100 nM Batabulin, approximately 50-80% of the cell population is undergoing apoptosis 1.Batabul

5、in (T138067) binds covalently and selectively to a subset of the -tubulin isotypes, thereby disruptingmicrotubule polymerization. Covalent modification occurs at a conserved Cys-239 shared by the 1, 2, and4 tubulin isotypes. Cells exposed to Batabulin become altered in shape, indicating a collapse o

6、f thecytoskeleton, and show an increase in chromosomal ploidy 1.Cell Cycle Analysis 1Cell Line: MCF7 cellsConcentration: 30 nM, 100 nM and 300 nMIncubation Time: 24 hoursResult: Showed an arrest at the G2/M cell-cycle boundary.Apoptosis Analysis 1Cell Line: MCF7 cellsConcentration: 30 nM, 100 nM and

7、 300 nMIncubation Time: 24 hours or 48 hoursResult: 25-30% of cells showed the reduced DNA content characteristic of apoptotic cells.體內(nèi)研究 Batabulin (T138067; 40 mg/kg; intraperitoneal injection; once per week; on days 5, 12, and 19; male athymicnude mice) treatment impairs the growth of the drug-sen

8、sitive CCRF-CEM tumors 1.Animal Model: Male athymic nude mice (nu/nu) (6-8 week-old, 20-25 g) injected withCCRF-CEM cells1Dosage: 40 mg/kgAdministration: Intraperitoneal injection; once per week; on days 5, 12, and 19Result: Impaired the growth of the drug-sensitive CCRF-CEM tumors.REFERENCES1. Shan

9、 B, et al. Selective, covalent modification of beta-tubulin residue Cys-239 by T138067, an antitumor agent with in vivo efficacyagainst multidrug-resistant tumors. Proc Natl Acad Sci U S A. 1999 May 11;96(10):5686-91.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product has not been fully validated for medical