Zenocutuzumab-MCLA-128-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZenocutuzumabCat.No.:HY-P99507CASNo.:1969309-56-5Synonyms:MCLA-128;PB4188;R040517作⽤靶点:EGFR作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Zenocutuzumab(MCLA-128)⼀种双特异性⼈化IgG1抗体，包含两个不同的Fab臂，靶向HER2和HER3的细胞外结构域。体外研究Zenocutuzumab(0.001-1000nM;96hours)inhibitscellgrowthinlungandbreastcancercelllines[1].Zenocutuzumab(0.1-1000nM;24hours)inhibitsHER3andAKTphosphorylation,inducesmarkersofapoptosisandcellcyclearrestinlungandbreastcancercelllines[1].CellViabilityAssay[1]CellLine:Humanbronchiolarepithelialcelllines(HBEC)Concentration:0.001nM,0.01nM,0.1nM,1nM,10nM,100nM,1000nMIncubationTime:96hResult:ReducedthegrowthofisogenicHBECexpressingeitherCD74-NRG1orVAMP2-NRG1fusions.WesternBlotAnalysis[1]CellLine:HBEC-CD74-NRG1,LUAD-0061AS3,MDA-MB-175-VIIcellsConcentration:0.1nM,1nM,10nM,100nM,1000nMIncubationTime:24hours1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:InhibitedHER3,STAT3,AKT,p70S6K,andS6phosphorylation.体内研究Zenocutuzumab(2.5-25mg/kg;i.p.;onceweekly;for28days)causesastatisticallysignificantreductionofgrowth,includingtumorregression[1].AnimalModel:6to12-week-oldfemaleNSG™(LUAD-0061AS3),BALB/cnude(OV-10–0050)orathymicnude(ST2891,ST3204andCTG-0953)miceinjectedwithNRG1fusion-positivepatient-derivedxenograft(PDX)tumors[1].Dosage:2.5mg/kg,8mg/kg,or25mg/kgAdministration:i.p.;onceweekly;for28daysResult:BlockedgrowthoflungandovariancancerPDXmodels.REFERENCES[1].AlisonMSchram,etal.Zenocutuzumab,aHER2xHER3BispecificAntibody,IsEffectiveTherapyforTumorsDrivenbyNRG1GeneRearrangements.CancerDiscov.2022May2;12(5):1233-1247.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400