Aprutumab-ixadotin-BAY-1187982-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAprutumabixadotinCat.No.:HY-141600CASNo.:1708947-48-1Synonyms:BAY1187982作⽤靶点:Antibody-DrugConjugates(ADCs);FGFR作⽤通路:Antibody-drugConjugate/ADCRelated;ProteinTyrosineKinase/RTK储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Aprutumabixadotin(BAY1187982)⾸个靶向FGFR2的抗体药物偶联物(ADC)，也⾸个使⽤奥⽿他汀基有效载荷的抗体药物偶联物。体外研究Aprutumabixadotin(0.097-0.83nM;72h)exhibitsantigenbindingaffinityof0.29nMagainstFGFR2,andshowsinhibitoryactivitiesinseveralcelllineswithIC50sof0.097-0.83nM[1].AprutumabixadotininducesapoptosisinvitrospecificallyinFGFR2-positivecells(SUN-52PE,SUN-16)[1].CellViabilityAssay[1]CellLine:SNU-16,KATOIII,SUM-52PE,NCI-H716,andMFM-223cells;MDA-MB-231cells;KYSE-180cells;4T1cellsConcentration:0.097-0.83nMIncubationTime:72hoursResult:Inhibitedcellviability.体内研究Aprutumabixadotin(5mg/kgand7.5mg/kg;i.v.;onceweeklyfor30d)iswelltolerated,andresultsinpartialtumorregressioninSNU-16,MFM-223orNCI-H716xenograftmodelsinmice[1].AnimalModel:SNU-16xenograftmodelinfemaleNODscidmiceandMFM-223andNCI-H716xenograftmodelsinfemaleNMRInu/numice[1]Dosage:0.5mg/kg,1mg/kg,5mg/kg,7.5mg/kg,15mg/kg1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Intravenousinjection;onceweeklyfor4weeksResult:Significantlytumorgrowthatleast90%at5mg/kginSNU-16xenograftmodel.However,dosesof0.5or1mg/kgdidnotsignificantlyinhibittumorgrowthcomparedtothevehiclecontrol.Markeddecreaseintumorvolumeat1and5mg/kginMFM-223model.Resultedinnotableinhibitionoftumorgrowthat7.5mg/kgincelllinederivedxenograftmodeloverexpressingFGFR2,theNCI-H716humancolorectalcancermodel.REFERENCES[1].SommerA,etal.PreclinicalEfficacyoftheAuristatin-BasedAntibody-DrugConjugateBAY1187982fortheTreatmentofFGFR2-PositiveSolidTumors.CancerRes.2016Nov1;76(21):6331-6339.[2].KimSB,etal.First-in-HumanPhaseIStudyofAprutumabIxadotin,aFibroblastGrowthFactorReceptor2Antibody-DrugConjugate(BAY1187982)inPatientswithAdvancedCancer.TargetOncol.2019Oct;14(5):591-601.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc