A-1331852 - Bcl-xL 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEA-1331852Cat. No.: HY-19741CAS No.: 1430844-80-6分式: CHNOS分量: 658.81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 (75.89 mM)H2O : 40% PEG300 5% Twee

2、n-80 45% salineSolubility: 2.5 mg/mL (3.79 mM); Suspended solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.79 mM); Suspended solution; Need ultrasonic1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.79 mM);

3、Clear solutionBIOLOGICAL ACTIVITY物活性 A-1331852具有服活性的BCL-XL选择性抑制剂，Ki值于10 pM。IC50 & Target Bcl-xL Bcl-W Bcl-2 Mcl-10.01 nM (Ki) 4 nM (Ki) 6 nM (Ki) 142 nM (Ki)体外研究 A-1331852 selectively disrupts BCL-XLBIM complexes and induces the hallmarks of apoptosis in BCL-XLdependent Molt-4 cells with IC50s in th

4、e low nanomolar range but does not affect MEF cells lacking BAKor BAX. In CellTiter-Glo cell viability assay, A-1331852 inhibits NCI-H847, NCI-H1417, SET-2, HEL, OCI-M2with EC50 values of 3, 7, 80, 120 and 100 nM 1.体内研究 A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducin

5、g tumor regressions as asingle agent. Additionally, A-1331852 combines with venetoclax to recapitulate the efficacy of navitoclax inthe NCI-H1963.FP5 xenograft model of SCLC. A-1331852 significantly inhibits tumor growth in sevensubcutaneous xenograft models of solid tumors, including breast cancer,

6、 NSCLC, and ovarian cancer 1.PROTOCOLCell Assay 1 SCLC and AML cell lines are incubated with increasing concentrations of navitoclax, venetoclax, or A-1155463 for 48 hours before assessing cell viability. Cell killing EC50 values are calculated 1.MCE has not independently confirmed the accuracy of t

7、hese methods. They are for reference only.Animal Mice: The growth inhibition of established tumors in SCID-bg mice is studied. A-1331852 is administeredAdministration 1 orally daily for 14 days at 25 mg/kg and docetaxel is administered intravenously at 7.5 mg/kg. The change oftumor volume is monitor

8、ed daily 1.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. Cell Death Dis. 2019 May 21;10(6):395.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies forcancer therapy. Sci Transl Med. 2015 Mar 18;7(279):279ra40.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCaution: Product has not been fully validated for medical ap