IACS-10759-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIACS-10759Cat. No.: HY-112037CAS No.: 1570496-34-2分式: CHFNOS分量: 562.56作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 62.5 mg/mL (111.10 mM; Need ultrasonic)H2O : 40%

2、PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.70 mM); Suspended solution; Need ultrasonic2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.70 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 IACS-10759是氧化磷酸化 (OXPHOS) 復(fù)合物I的有效抑制劑。IC50 & Tar

3、get OXPHOS 1體外研究 IACS-10759 inhibits the conversion of NADH to NAD+ in an immunoprecipitated complex I assay at low nMconcentrations 1.體內(nèi)研究 IACS-10759 is orally bioavailable with excellent physicochemical properties in preclinical species andachieves significant in vivo efficacy with daily oral dosi

4、ng of 10-25 mg/kg. There is a 50 day extension ofmedian survival in an orthotopic AML cell line xenograft and robust regression in DLBCL and GBM xenograftmodels 1.REFERENCES1. Protopopova M. IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. abstract.

5、In:Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia(PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 4380. doi:10.1158/1538-7445.AM2015-4380McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021-58