SIAIS562055-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESIAIS562055Cat.No.:HY-168637分?式:C??H??F?N?O?S分?量:918.12作?靶點(diǎn):PROTACs;Ras作?通路:PROTAC;GPCR/GProtein;MAPK/ERKPathway儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性SIAIS562055?種有效的于cereblon的SOS1PROTAC，Kd為95.9nM。SIAIS562055表現(xiàn)出持續(xù)降解SOS1和抑制下游ERK通路。SIAIS562055有效阻斷了KRASG12C或KRASG12D與SOS1的結(jié)合，IC50值分別為95.7nM和134.5nM。SIAIS562055表現(xiàn)出強(qiáng)?的抗癌活性。（粉?：SOS1配體(HY-168638)；??：連接?(HY-W539874)；藍(lán)?：E3連接酶配體(HY-W076696)）。IC50&TargetCereblonSOS195.9nM(Kd)體外研究SIAIS562055(10-1000nM;24h)exhibitssustaineddegradationofSOS1andinhibitionofdownstreamERKpathways,resultinginsuperioranti-proliferativeactivitycomparedtosmallmoleculeinhibitors[1].WesternBlotAnalysis[1]CellLine:NCI-H358andGP2dcellsConcentration:10nM,100nM,1000nMIncubationTime:24hResult:ExhibitedsustaineddegradationofSOS1andinhibitionofdownstreamERKpathways.體內(nèi)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?邊的抑制劑?師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