4A-BFA-11-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE4A-BFA-11Cat.No.:HY-180557分⼦式:C₁₁₃H₁₇₃N₂₃O₃₁分⼦量:2349.72作⽤靶点:FolateReceptor(FR)作⽤通路:CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性4A-BFA-11⼀种叶酸靶向PEG-MMAE偶联物，对叶酸受体α(FR-α)具有特异性结合亲和⼒(KD=106.7nM)。4A-BFA-11通过结合聚⼄⼆醇(PEG)介导的长循环(EPR效应)和叶酸受体靶向作⽤，实现肿瘤富集。4A-BFA-11在肿瘤部位发⽣酶切，释放活性有效载荷，从⽽实现精准作⽤。4A-BFA-11在HeLa⼩⿏模型中，能⾼效地携带、靶向并控制MMAE在肿瘤组织中的释放。4A-BFA-11可⽤于宫颈癌、巢癌和肺癌的研究[1]。IC50&TargetFR-α106.7nM(Kd)体外研究4A-BFA-11(72h)exhibitsantiproliferationactivityinHeLa,SK-OV-3,andA549cells,withIC50sof37.62,28.8,and15.1nM,respectively[1].体内研究4A-BFA-11(0.4and0.8mg/kg,i.v.,onceweeklyfor2weeks)inhibitstumorgrowthinaHeLamousecervicalcancermodel[1].AnimalModel:BALB/cnudemice(5-6weeks)inoculatedwithHeLagrafttumorsintherightaxilla[1]Dosage:0.4and0.8mg/kgAdministration:i.v.,onceweeklyfor2weeksResult:Resultedinstrongerantitumoreffectswithatumorgrowthinhibitionrate(T/C%)of67.1%at0.4mg/kg.AchievedpronouncedantitumoreffectswithaT/C%of95.9%at0.8mg/kg.Showednosignificantbodyweightlossandnosignificantchangesinbloodparameters.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEInducedmildhepatitisat0.4mg/kg,characterizedbytraceinflammatorycellinfiltrationpredominantlycomposedoflymphocytesandgranulocytes.Exhibitedmildsinusoidaldilatationinthespleen,andthelow-dosegroupshowedslightadhesionofthewhitepulp.REFERENCES[1].BaiL,etal.DesignandEvaluationofaFolate-TargetedPEG-MMAEConjugatewithEnzyme-ActivatedDrugReleaseforEnhancedTumorSelectivityandAntitumorEfficacy.JMedChem.2025Dec25;68(24):26579-26591.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-