Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAGS-16C3FCat.No.:HY-171544Synonyms:AGS-16M8F作?靶點:Antibody-DrugConjugates(ADCs);Phosphodiesterase(PDE)作?通路:Antibody-drugConjugate/ADCRelated;MetabolicEnzyme/Protease儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性AGS-16C3F?種靶向ENPP3的抗體-藥物偶聯物(ADC)。AGS-16C3F由靶向ENPP3的Anti-ENPP3/CD203cAntibody(HY-P990315)通過連接?與MonomethylauristatinF(HY-15579)連接?成。AGS-16C3F具有抗腫瘤活性，可?于轉移性腎細胞癌(mRCC)的研究[1][2]。IC50&TargetPDE3體外研究AGS-16C3F(0.001-1350nM,96h)hasIC50of1.1nM,2.73nM,109.9nMand146.5nMinROSAKITD816V,ROSAKITD816V-Gluc,HMC-1.1andHMC-1.2cells,respectively,showspotentinhibitoryactivityagainsttheproliferationofROSAcellswithhighexpressionofCD203c[2].AGS-16C3F(0.5-100nM,96-120h)inducesapoptosisandkillstumorcellswithhighexpressionofCD203cinROSAKITD816V,ROSAKITD816V-Gluc,HMC-1.1andHMC-1.2cells[2].ApoptosisAnalysis[2]CellLine:ROSAKITD816V,ROSAKITD816V-Gluc,HMC-1.1andHMC-1.2cellsConcentration:0.5-100nMIncubationTime:96-120hResult:SignificantlyincreasedtheproportionofapoptoticcellsinROSAcells(dose-dependent).HadalowapoptosisrateinHMC-1cells.體內研究AGS-16C3F(1,4mg/kg,i.v.onceevery4days,4timesintotal)significantlyreducestumorburdenandprolongssurvivalintheNOD-SCIDγmicemodeltransplantswithROSAKITD816V-Gluccellswithout1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEsignificanttoxicity[2].AnimalModel:NOD-SCIDγmiceinjectedwithROSAKITD816V-Gluc(5millioncells)[2]Dosage:1,4mg/kgAdministration:i.v.onceevery4days,4timesintotalResult:Significantlyreducedthenumberoftumorcellsinperipheralblood,bonemarrow,andspleen,anddecreasedserumtryptaselevels.Duringtreatmentandafterdrugwithdrawal,theluciferaseactivity(markeroftumorburden)ofmiceinthehigh-dosegroupcontinuedtobelowerthanthatinthecontrolgroup,anddiseaserecurrencewasdelayed.Significantlyprolongedthesurvivalofmice.Showedasignificantincreaseinapoptoticcellsinthemousebonemarrow,indicatingthattheanti-tumoreffectwasmainlyachievedbyinducingapoptosis.REFERENCES[1].KollmannsbergerC,etal.ARandomizedPhaseIIStudyofAGS-16C3FVersusAxitinibinPreviouslyTreatedPatientswithMetastaticRenalCellCarcinoma.Oncologist.2021Mar;26(3):182-e361.[2].ZhangY,etal.Invitroandinvivoefficacyofananti-CD203cconjugatedantibody(AGS-16C3F)inmousemodelsofadvancedsystemicmastocytosis.BloodAdv.2019Feb26;3(4):633-643.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic