ARQ-069-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesARQ069Cat.No.:HY-101544CASNo.:1314021-57-2分?式:C??H??N?分?量:273.33作?靶點(diǎn):FGFR作?通路:ProteinTyrosineKinase/RTK儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性ARQ069ARQ523的類似物，以對映體特異的?式抑制FGFR活性。ARQ069靶向?磷酸化，?活性形式的FGFR1/FGFR2激酶，IC50分別為0.84μM和1.23μM。ARQ069通過?ATP競爭的?式抑制FGFR1/FGFR2?磷酸化，IC50分別為2.8μM和1.9μM。IC50&TargetunphosphorylatedunphosphorylatedFGFR1FGFR2FGFR1FGFR2autophosphorylationautophosphorylation0.84μM(IC50)1.23μM(IC50)2.8μM(IC50)1.9μM(IC50)體外研究ARQ069(3.8-60μM;for2hours)reducesthedegreeofphosphorylationofFGFR(predominantlyFGFR2)inaconcentration-dependentmanner,withoutdecreasingβ-actin[1].ARQ069showsanaffinityforFGFR2of5.2μM[1].ARQ069inhibitsFGFRphosphorylationinKatoIIIcellswithanIC50of9.7μM[1].ARQ069targetstheinactiveformsofFGFR1andFGFR2kinasesandinhibitstheirenzymaticactivity.WhenARQ069ispreincubatedwitheitherphosphorylatedFGFR1orFGFR2,thepotencyofARQ069ininhibitingPyk2phosphorylationismarkedlyreduced,withIC50valuesdeterminedtobegreaterthan30and24.8μMforFGFR1andFGFR2,respectively.ARQ069exhibitsatleasta20-foldpreferenceforbindingtotheunphosphorylated,inactiveformsofFGFR1andFGFR2[1].ARQ068istheR-enantiomer,andARQ069istheS-enantiomer[1].WesternBlotAnalysis[1]CellLine:KatoIIIhumangastriccarcinomacellsConcentration:3.8,7.5,15,30,60μM1/2IncubationTime:For2hoursResult:ReducedthedegreeofphosphorylationofFGFR(predominantlyFGFR2)inaconcentration-dependentmanner,withoutdecreasingβ-actin.REFERENCES[1].EathirajS,etal.Anovelmodeofproteinkinaseinhibitionexploitinghydrophobicmotifsofautoinhibitedkinases:discoveryofATP-independentinhibitorsoffibroblastgrowthfactorreceptor.JBiolChem.2011Jun10;286(23):20677-87.McePdfHeightMedChemExpress(MCE)只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或藥證申報(bào)的