BAY-1135626-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBAY1135626Cat.No.:HY-147281CASNo.:1404071-37-9分⼦式:C₅₅H₈₆N₁₀O₁₁分⼦量:1063.33作⽤靶点:Others作⽤通路:Others储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性BAY1135626⽤于合成BAY1129980，⽤于抗肿瘤研究。BAY1129980⼀种于Auristatin的ADC试剂，具有抗C4.4A(LYPD3)作⽤，可⽤于⾮⼩细胞肺癌(NSCLC)的研究。体外研究C4.4A(LYPD3)isaproteinexpressedinnon-smallcelllungcancer(NSCLC),withscarcelyexpressinginnormaltissues[1].BAY1135626canbesynthesizedintoBAY1129980(C4.4A-ADC),showsastronganti-proliferativeeffectonC4.4Aexpressingcelllines[1].BAY1129980(0.001-100nM;72h)inhibitstheproliferationofA549lungcancercelllinestransfectedwithC4.4A[1].BAY1129980(0.001-100nM;72h)exhibitshighandselectiveefficacyonhC4.4A:A549cellsinvitro[1].CellCytotoxicityAssay[1]CellLine:hC4.4A:A549lungcancercellsConcentration:0.001-100nMIncubationTime:72hoursResult:HighpotencyatsubnanomolarrangewithanIC50valueof0.05nM.ResultedremarkableselectivityonhC4.4A:A549withover1,000-foldcomparedwithmock:A549cells.CellViabilityAssay[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:NCI-H292,FaDu,NCI-H322,SCaBER,SCC-4Concentration:0.001-100nMIncubationTime:72hoursResult:Inhibitedcancercellgrowthinadose-dependentmanner.体内研究BAY1129980(1.9-7.5mg/kg;i.v.;20d)inhibitstumorgrowthinvivoinmouse[1].BAY1129980witharepeateddosing(15mg/kg;i.v.;21dfor1stcycleand57dfor2ndcycle)iswelltoleratedwithoutchangingthesensitivitytothetreatment[1].AnimalModel:C4.4A-positiveNCI-H292NSCLCxenograftmousemodel[1]Dosage:1.9,3.75,7.5mg/kgAdministration:Intravenousinjection;20daysResult:Haltedtumorgrowthonday20dosedependently,asthemonotherapytreatment,withaminimumeffectivedose(MED)of1.9mg/kg.AnimalModel:C4.4A-positiveNCI-H292NSCLCxenograftmousemodel[1]Dosage:15mg/kgAdministration:Intravenousinjection;21daysforthefirstcycleteament,57daysforthesecondcycletreatmentResult:Reducedtumorvolumewithamarkeddelayoftumorgrowth.Demonstratedwelltolerance,stillleftregrowntumorssensitivetotreatment.REFERENCES[1].WilludaJ,etal.PreclinicalAntitumorEfficacyofBAY1129980-aNovelAuristatin-BasedAnti-C4.4A(LYPD3)Antibody-DrugConjugatefortheTreatmentofNon-SmallCellLungCancer.MolCancerTher.2017May.16(5):893-904.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.