Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemECE-355621Cat.No.:HY-P991565作用靶點(diǎn): c-Met/HGFR作用通路: ProteinTyrosineKinase/RTK儲(chǔ)存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性CE-355621是一種人源化的抗c-MetIgG1單克隆抗體。CE-355621在A(yíng)549細(xì)胞中能有效地與人c-Met結(jié)合(KD=200pM,IC50=466pM)，在食蟹猴腎細(xì)胞中能與食蟹c-Met有效結(jié)合(KD=610pM)。CE-355621通過(guò)阻斷HGF結(jié)合來(lái)抑制c-Met信號(hào)通路。CE-355621顯著抑制依賴(lài)c-Met/HGF途徑的腫瘤生長(zhǎng)。CE-355621可用于膠質(zhì)母細(xì)胞瘤和胃癌等癌癥的研究[1][2]。IC50&Targetc-Met體外研究CE-355621(0.01-100nM,4h)canefficientlyblockthebindingofc-MettoHGFandinducec-MetdegradationinA549cells[1].CE-355621(0.01nM-10nM,24h)significantlyinhibitsc-MetactivationinU87MGcells[1].CE-355621(0.01-10μg/mL,48h)caninducec-MetdegradationinU87MGcells[1].WesternBlotAnalysis[1]CellLine:U87MGcellsConcentration:0.01nM-10nMIncubationTime:24hResult:Significantlyinhibitedactivationofc-Met.WesternBlotAnalysis[1]CellLine:U87MGcells1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEConcentration:0.01-10μg/mLIncubationTime:48hResult:Reducedthelevelofc-Met.體內(nèi)研究CE-355621(25-200μg,i.p.,onday0,2,3,6and8)significantlydelaystumorgrowthinfemaleCD-1nu/numicebearingU87MGxenografts[1].CE-355621(400μg,i.p.,onday7and14)significantlyinhibitstumorgrowthinfemaleCD-1nu/numicebearingGTL-16xenografts[1].CE-355621(200μg,i.p.,singledose,onday7)caneffectivelyinhibittumorvolumegrowthanduptakeof18F-FDGinfemalenude(nu/nu)micebearingU87MGxenografts[2].AnimalModel:5×106U87MGcellsinjectedfemaleCD-1nu/numice[1]Dosage:25,100and200μgAdministration:Intraperitonealinjection(i.p.)onday0,2,3,6and8Result:Significantlydelayedtumorgrowth(upto22.3days)andinhibited80%ofc-Metphosphorylation.AnimalModel:1.0-5.0×106GTL-16cellsinjectedfemaleCD-1nu/numice[1]Dosage:400μgAdministration:Intraperitonealinjection(i.p.)onday7and14Result:Inhibitedtumorgrowthby85%andreducedc-Metphosphorylationby48%AnimalModel:1×106U87MGcellsinjectedfemalenude(nu/nu)mice[2]Dosage:200μgAdministration:Intraperitonealinjection(i.p.),singledoseonday7Result:Significantlyinhibitedtumorvolume.Significantlyreduceduptakeof18F-FDG.REFERENCESMichaudNR,etal.Biochemicalandpharmacologicalcharacterizationofhumanc-MetneutralizingmonoclonalantibodyCE-355621.MAbs.2012Nov-Dec;4(6):710-23.TsengJR,etal.Preclinicalefficacyofthec-MetinhibitorCE-355621inaU87MGmousexenograftmodelevaluatedby18F-FDGsmall-2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEanimalPET.JNuclMed.2008Jan;49(1):129-134.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapp