Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESotorasib-d3Cat.No.:HY-114277S2Synonyms:AMG-510-d3分?式:C??H??D?F?N?O?分?量:563.61作?靶點:Isotope-LabeledCompounds;Ras作?通路:Others;GPCR/GProtein;MAPK/ERKPathway儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Sotorasib-d3(AMG-510-d3)氘代標記的Sotorasib.Sotorasib(AMG-510)?種有效的，?服?物可利?的，選擇性的KRASG12C共價抑制劑。Sotorasib將KRASG12C鎖定在?活躍的GDP約束狀態。Sotorasib導致KRASG12C突變的局部晚期或轉移性??細胞肺癌(NSCLC)的消退[1][2][3][4][5][6]。體外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.REFERENCES[1].RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019;53(2):211-216.[2].WuLL,etal.AMG-510andcisplatincombinationincreasesantitumoreffectinlungadenocarcinomawithmutationofKRASG12C:apreclinicalandtranslationalresearch.DiscovOncol.2023Jun7;14(1):91.[3].RyanMB,etal.KRASG12C-independentfeedbackactivationofwild-typeRASconstrainsKRASG12Cinhibitorefficacy.CellRep.2022Jun21;39(12):110993.[4].MarwanFakih,etal,Phase1studyevaluatingthesafety,tolerability,pharmacokinetics(PK),andefficacyofAMG510,anovelsmallmoleculeKRASG12Cinhibitor,inadvancedsolidtumors.JournalofClinicalOncology.[5].KarenRex,etal.Abstract3090:InvivocharacterizationofAMG510-apotentandselectiveKRASG12CcovalentsmallmoleculeinhibitorinpreclinicalKRASG12Ccancermodels.ExperimentalandMolecularTherapeutics.[6].BrianA.Lanman,etal.Abstract4455:DiscoveryofAMG510,afirst-in-humancovalentinhibitorofKRASG12Cforthetreatmentofsolidtumors.CancerChemistry.[7].CanonJ,etal.TheclinicalKRAS(G12C)inhibitorAMG510drivesanti-tumourimmunity.Nature.2019Nov;575(7781):217-223.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon