INCB3619-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEINCB3619Cat.No.:HY-12636CASNo.:791826-72-7分?式:C??H??N?O?分?量:413.47作?靶點(diǎn):MMP;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性INCB3619?種選擇性的，具有?服活性的ADAM抑制劑，作?于ADAM10和ADAM17的IC50值分別是22nM和14nM。INCB3619具有抗腫瘤活性。體外研究INCB3619(0-10μM,96h)caninhibitheregulin-dependentHER3-Aktpathway,butnotERKactivityinA549cells,andinduceapoptosisinA549cells[1].INCB3619(0-10μM,72h)caninhibitEGFRligandsignalingintheEGFRautocrinecelllineNCI-H1666andcanbeusedincombinationwithotheranti-EGFRdrugssuchasgefitinib[1].INCB3619(2μM)inhibitsERK1/2expressioninNCI-H1666andmakeitsensitivetoGefitinib(HY-50895)[1].ApoptosisAnalysis[1].CellLine:A549cellConcentration:1,10μMIncubationTime:Result:Inducedabout3%apoptosisataconcentrationof1μMandabout5%ataconcentrationof10μM.CellViabilityAssay[1].CellLine:NCI-H1666cellConcentration:0-10μM1/2www.MedChemEIncubationTime:72hResult:InhibitedproliferationofNCI-H1666cells.體內(nèi)研究INCB3619(subcutaneousinjection,60mg/kg/d,14d)exhibitsantitumoractivityandsensitizestumorstoGefitinib(HY-50895)inA549xenograftedBALB/cnu/numousemodel[1].AnimalModel:BALB/cnu/numousemodelofA549xenograftDosage:50,60mg/kgAdministration:subcutaneousinjection,daily,14dResult:Significanttumorgrowthinhibitionanddelayat60mg/kgdose,lessactiveeffectat50mg/kg.REFERENCES[1].Bin-BingSZhou,etal.TargetingADAM-mediatedligandcleavagetoinhibitHER3andEGFRpathwaysinnon-smallcelllungcancer.CancerCell.2006Jul;10(1):39-50.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications