KRASG12C-IN-18-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKRASG12CIN-18Cat.No.:HY-179404CASNo.:2966924-24-1分⼦式:C₃₇H₃₂F₄N₆O₂分⼦量:668.68作⽤靶点:Ras作⽤通路:GPCR/GProtein;MAPK/ERKPathway储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性KRASG12CIN-18⼀种⼝服活性的KRASG12C共价抑制剂，可在GDP与GMPPNP结合状态下实现对KRASG12C的完全共价结合，并对KRASG12C及其耐药相关突变体（包括KRASG12C/R68S）表现出显著的抗增殖活性，IC50为低纳尔⽔平。KRASG12CIN-18在KRASG12C驱动的实体瘤及KRASG12C/R68S异种移植模型中表现出显著的体内活性，可⽤于直肠腺癌研究[1]。IC50&TargetKRAS(G12C)(IC50)体外研究Following72-144hincubation,KRASG12CIN-18(compound20)potentlyinhibitedKRASG12C-mutantBa/F3cellsandmultiplesecondaryresistancevariants,includingH95Q(IC50=7.5nM),Y96D(IC50=2.8nM),R68S(IC50=5.4nM)andQ99L(IC50=8.2nM),showinglow-nanomolarinhibitoryactivityacrossthesemodels[1].KRASG12CIN-18achieves100%covalentmodificationofKRASG12CinbothGDP-boundandGMPPNP-boundstateswithinminutes,indicatingrapidandefficienttargetengagement[1].体内研究KRASG12CIN-18(SW837KRASG12Crectalcancerxenograft;oraladministration,30mg/kg,oncedaily,28days)demonstratesrobustantitumorefficacy,achievingcompletetumorstasiswith103%tumorgrowthinhibitionandexceedingtheactivityofMRTX849andAMG510[1].KRASG12CIN-18(Ba/F3KRASG12C/R68Sxenograft;oraladministration,30mg/kg,oncedaily,21days)alsoshowsstrongantitumoractivity,producing79.2%tumorregressionandexhibitinggoodtolerability[1].AnimalModel:SW837humanrectalcancerxenograft(KRASG12C)femaleNODSCIDmice(6–71/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEweeksold,20.5-23.7g)Dosage:30mg/kgAdministration:Oralgavage(p.o.);oncedaily;28daysResult:Achieved103%tumorgrowthinhibitionandinducedcompletetumorstasiswithoutbody-weightloss.AnimalModel:Ba/F3KRASG12C/R68SxenograftmodelfemaleNODSCIDmice(6-8weeksold,18.6-23.3g)Dosage:30mg/kgAdministration:Oralgavage(p.o.);oncedaily;21daysResult:Produced79.2%tumorregressionanddemonstratedgoodtolerability.REFERENCES[1].GaoK,etal.Structure-baseddesignandsynthesisofnovelhighlypotentandselectiveKRASG12Cinhibitors.EurJMedChem.2026;302(Pt2):118321.doi:10.1016/j.ejmech.2025.118321McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc