A-1155463 - Bcl-2 Family 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEA-1155463Cat. No.: HY-19725CAS No.: 1235034-55-5分式: CHFNOS分量: 669.79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 DMSO : 50 mg/mL (74.65 mM; Need ultrasonic)H2O :

2、40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.73 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.73 mM); Suspended solution; Need ultrasonic3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/

3、mL (3.73 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 A-1155463效选择性的 BCL-XL 抑制剂，在Molt-4细胞中的EC50值为70 nM。IC50 & Target Bcl-xL Bcl-20.01 nM (Ki) 80 nM (Ki)体外研究 A-1155463 shows picomolar binding affinity to BCL-XL (Ki0.01 nM), and 1000-fold weaker binding toBCL-2 (Ki= 80 nM) and related proteins BCL-W (Ki=

4、 19 nM) and MCL-1 (Ki 440 nM) 2. A-1155463demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC50 values0.5 M in the presence of 10 % FBS 3.体内研究 A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 smallcell lung can

5、cer xenograft tumor growth in vivo following multiple doses 2.PROTOCOLAnimal Mice: Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, plateletAdministration 2 counts fell dramatically as measured at 6 h postdose and then rebounded to normal levels within 72 h. A-115

6、5463 is then administered to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146tumor cells with a daily dose at 5 mg/kg IP for 14 days 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Immunity. 2019 May. Oncogene. 2019 Jan;

7、38(1):47-59. Cell Death Dis. 2019 May 21;10(6):395. Immunol Cell Biol. 2018 Oct;96(9):912-921. Leuk Lymphoma. 2019 Jan 10:1-11.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies

8、and define improved strategies forcancer therapy. Sci Transl Med.?2015 Mar 18;7(279):2792. Tao ZF, et al. Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93.3. Zhang H, et al. Genomic analysis and selective small molecule inhibition identifies BCL-X(L) as a critical survival factor in a subset of2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEcolorectal cancer. Mol Cancer. 2015 Jul 2;14:126.McePdfHeightCaution: Product has not been fully validated for medical appl