SIAIS562055-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESIAIS562055Cat.No.:HY-168637分⼦式:C₄₉H₆₂F₃N₇O₅S分⼦量:918.12作⽤靶点:PROTACs;Ras作⽤通路:PROTAC;GPCR/GProtein;MAPK/ERKPathway储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性SIAIS562055⼀种有效的于cereblon的SOS1PROTAC，Kd为95.9nM。SIAIS562055表现出持续降解SOS1和抑制下游ERK通路。SIAIS562055有效阻断了KRASG12C或KRASG12D与SOS1的结合，IC50值分别为95.7nM和134.5nM。SIAIS562055表现出强⼤的抗癌活性。（粉⾊：SOS1配体(HY-168638)；⿊⾊：连接⼦(HY-W539874)；蓝⾊：E3连接酶配体(HY-W076696)）。IC50&TargetCereblonSOS195.9nM(Kd)体外研究SIAIS562055(10-1000nM;24h)exhibitssustaineddegradationofSOS1andinhibitionofdownstreamERKpathways,resultinginsuperioranti-proliferativeactivitycomparedtosmallmoleculeinhibitors[1].WesternBlotAnalysis[1]CellLine:NCI-H358andGP2dcellsConcentration:10nM,100nM,1000nMIncubationTime:24hResult:ExhibitedsustaineddegradationofSOS1andinhibitionofdownstreamERKpathways.体内研究SIAIS562055(20-50mg/kg;ip;daily;for3weeks)displaysapromisingantitumorpotencyinKRAS-mutantxenografts[1].AnimalModel:FemaleBALB/cmice(6-7-week-old)injectedwithMIAPaCa-2cells[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:20mg/kg;40mg/kg;50mg/kgAdministration:ip;daily;for3weeksResult:Displayedpromisingantitumorpotency.REFERENCES[1].ZiweiLuo,etal.TargetedDegradationofSOS1ExhibitsPotentAnticancerActivityandOvercomesResistanceinKRAS-MutantTumorsandBCR-ABL-PositiveLeukemia.CancerRes.2024Oct22.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-58