Navitoclax-ABT-263-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENavitoclaxCat. No.: HY-10087CAS No.: 923564-51-6Synonyms: ABT-263分式: CHClFNOS分量: 974.61作靶点: Bcl-2 Family作通路: Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMF : 100 mg/mL (102.61 mM)DMS

2、O : 75 mg/mL (76.95 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.57 mM); Suspended solution; Need ultrasonic1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.57 mM); Clear solutionBIOLOGICAL ACTIVITY物活性

3、 Navitoclax (ABT-263)有效，可服的 Bcl-2 抑制剂，可与Bcl-xL，Bcl-2， Bcl-w等多种Bcl-2家族蛋结合，Ki 值于 1 nM。IC50 & Target Bcl-W Bcl-xL Bcl-21 nM (Ki) 1 nM (Ki) 1 nM (Ki)体外研究 Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. Themedian IC50 for all of the lines in the

4、 panel is 1.91 M 1. Navitoclax in combination with chemotherapyagents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation inboth SK-OV-3 and IGROV-1 cell lines 2.体内研究 Navitoclax (100 mg/kg; orally; 21-day treatment) enhances the activity of OSI-744 in viv

5、o. As a single agent,100 mg/kg Navitoclax alone dosed daily has no significant antitumor activity, whereas daily dosing of OSI-744 at 50 mg/kg results in significant tumor stasis (%TGI=52) during a 21-day treatment period. Notably, thecombination of Navitoclax and OSI-744 dosed daily for 21 consecut

6、ive days results in 98% TGI and durabletumor regressions in 100% of treated tumor-bearing mice 3.Animal Model: Mice with NCI-H1650 model 3Dosage: 100 mg/kgAdministration: Orally; daily; for 21 consecutive daysResult: As a single agent, 100 mg/kg alone dosed daily had no significant antitumor activit

7、y.Notably, the combination with OSI-744 resulted in 98% TGI and durable tumorregressions in 100% of treated tumor-bearing mice.户使本产品发表的科研献 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Nat Commun. 2019 Feb 6;10(1):620. Cell Death Dis. 2019 Aug 9;10(8):602. Cell Death Dis. 2018 Sep 24;9(10):986

8、. Breast Cancer Res Treat. 2019 Feb;173(3):585-596.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Lock R1, et al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood C

9、ancer.2008 Jun;50(6):1181-1189.2. Wong M, et al. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models.Mol Cancer Ther. 2012Apr;11(4):1026-1035.3. Chen J, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. MolCancer Ther. 2011 Dec;10(12):2340-9.McePdfHeightCaution: Product has not been fully validated for me