KRASG12C-IN-17-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKRASG12CIN-17Cat.No.:HY-179403CASNo.:2966924-23-0分⼦式:C₃₇H₃₃F₃N₆O₂分⼦量:650.69作⽤靶点:Ras作⽤通路:GPCR/GProtein;MAPK/ERKPathway储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性KRASG12CIN-17⼀种具有⼝服活性的共价性KRASG12C抑制剂，并在KRASG12C突变的癌细胞中表现出强效的抑制活性（NCI-H23IC50=0.7nM；NCI-H358IC50=0.5nM)。KRASG12CIN-17可在GDP结合态与GMPPNP结合态下⾼效且不可逆地与KRASG12C形成共价结合，修饰率超过96%。KRASG12CIN-17可⽤于KRAS驱动的肿瘤研究，包括结直肠癌[1]。IC50&TargetKRasG12C体外研究KRASG12CIN-17(compound19)potentlyinhibitsKRASG12C-mutantNCI-H23andNCI-H358cellswithIC50valuesof0.7nMand0.5nM,respectively,following72-144hoursofincubation[1].KRASG12CIN-17covalentlymodifiesKRASG12CinbothGDP-andGMPPNP-boundstateswith>96%conjugationefficiencywithin15minutes[1].KRASG12CIN-17inhibitsmultipleresistance-associatedKRASG12Cvariants,includingR68S,H95Q,Y96CandQ99L,inBa/F3cells[1].KRASG12CIN-17exhibitsantiproliferativeactivityagainstselectedKRASG12Csecondary-mutationcancercelllines,retainingstrongpotencyparticularlyagainstY96CandQ99Lvariants[1].CellProliferationAssay[1]CellLine:NCI-H23(KRASG12C),NCI-H358(KRASG12C)Concentration:0.7nM(NCI-H23),0.5nM(NCI-H358)IncubationTime:72h1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:SignificantlyinhibitedproliferationofKRASG12C-mutantNCI-H23andNCI-H358cells.体内研究KRASG12CIN-17(30mg/kg,oralgavage,QDfor28days)demonstratesstronginvivoactivity,producing103%tumorgrowthinhibitioninSW837KRASG12Cxenograftmodels[1].KRASG12CIN-17(30mg/kg,oralgavage,QDfor21days)significantlyreducestumorvolumeinBa/F3KRASG12C/R68Sxenograftmodels,achieving65.9%tumorreduction[1]AnimalModel:SW837humanrectalcancerxenograft(KRASG12C)femaleNODSCIDmice(6–7weeksold,20.5–23.7g)Dosage:30mg/kgAdministration:Oralgavage(p.o.);oncedaily(QD);28daysResult:Achieved103%tumorgrowthinhibitionandinducednear-completetumorstasiswithoutsignificantbody-weightlossinSW837KRASG12Cxenograftmodels.AnimalModel:Ba/F3KRASG12C/R68SxenograftmodelfemaleNODSCIDmice(6-8weeksold,18.6-23.3g)Dosage:30mg/kgAdministration:Oralgavage(p.o.);oncedaily(QD);21daysResult:Reducedtumorvolumeby65.9%anddemonstratedgoodtolerabilityinBa/F3KRASG12C/R68Sxenograftmodels.REFERENCES[1].GaoK,etal.Structure-baseddesignandsynthesisofnovelhighlypotentandselectiveKRASG12Cinhibitors.EurJMedChem.2026;302(Pt2):118321.doi:10.1016/j.ejmech.2025.118321McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica