SOS1-IN-21-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemESOS1-IN-21Cat.No.:HY-175326CASNo.:2767633-04-3分子式:C₂₅H₃₀F₃N₃O₄分子量:493.52作用靶点:SOS1作用通路:MAPK/ERKPathway储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性SOS1-IN-21是一种口服有效的sonofSevenless1(SOS1)抑制剂，其IC50值为15nM。SOS1是一种鸟嘌呤核苷酸交换因子(GEF)，通过促进GDP到GTP的转换来激活KRAS。SOS1-IN-21具有强大的抗增殖活性，对NCI-H358细胞的IC50值为16nM，对MiaPaca-2细胞为17nM。SOS1-IN-21在MiaPaca-2肿瘤移植模型中表现出显著的抗肿瘤活性。SOS1-IN-21可用于研究KRAS突变肿瘤，如胰腺癌[1]。体外研究SOS1-IN-21(Compound21)(0-3000nM)significantlyenhancesgrowthsuppressioninMiaPaCa-2cellsincombinationoftheKRASG12CinhibitorAMG510(HY-114277)[1].体内研究SOS1-IN-21(Compound21)(12-50mg/kg,p.o.,twicedaily,for23days)significantlyinhibitstumorgrowthandtheeffectisenhancedwithAMG510inMiaPaCa-2xenograftmodel[1].AnimalModel:MiaPaCa-2tumorcellsinducedxenograftmodelestablishedinBALB/cnudemice[1]Dosage:12mg/kg(Day0-9)and50mg/kg(Day9-23)Administration:Oraladministration(p.o.),for23daysResult:Showedatumorinhibitionrateof38%attheendofthe23-day.ResultedinasynergisticeffectontumorcellgrowthinhibitionwithAMG510.REFERENCES[1].LvY,etal.APotentSOS1PROTACDegraderwithSynergisticEfficacyinCombinationwithKRASG12CInhibitor.JMedChem.20241/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEFeb22;67(4):2487-2511.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792/p>