KD36-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKD36Cat.No.:HY-179702分⼦式:C₂₉H₃₂N₆O₃分⼦量:512.6作⽤靶点:Ras;PERK;Akt;ReactiveOxygenSpecies(ROS);Apoptosis;MitochondrialMetabolism作⽤通路:GPCR/GProtein;MAPK/ERKPathway;CellCycle/DNADamage;PI3K/Akt/mTOR;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性KD36⼀种选择性KRAS-G12C抑制剂，其IC50值为0.92μM。KD36可抑制ERK和AKT的磷酸化，诱导活性氧(ROS)积累，降低线粒体膜电位，从⽽导致KRAS-G12C突变细胞凋亡(apoptosis)。KD36可⽤于⾮⼩细胞肺癌(NSCLC)的研究。IC50&TargetKRasG12C0.92μM(IC50)体外研究KD36(72h)demonstratespotentantiproliferativeactivityinKRAS-G12CmutantNCI-H23,NCI-H358cellswithIC50valuesof0.42and0.65μM[1].KD36(0.5-4.0μM;24-48h)inducesmitochondrial-dependentapoptosisbyincreasingintracellularROSlevelsandreducingmitochondrialmembranepotentialinNCI-H23cells[1].KD36(0.5-8.0μM;8h)significantlyinhibitsthephosphorylationofKRASdownstreameffectorsERKandAKT(p-ERK,p-AKT)inNCI-H23cells,withnoobviousinhibitoryeffectonKRASwild-type(NCI-H2228)cells[1].KD36(0.1-1.0μM,14days)dose-dependentlysuppressescolonyformationofNCI-H23andNCI-H358cells[1].WesternBlotAnalysis[1]CellLine:NCI–H23,NCI–H2228Concentration:0.5μM,1.0μM,2.0μM,4.0μM,8.0μM1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:8hResult:SignificantlyreducedthephosphorylationofERKandAKTinNCI-H23cells,witha80%reductioninpERKand70%reductioninpAKTat4.0μM.Immunofluorescence[1]CellLine:NCI–H23cellsConcentration:0.5μM,1.0μM,2.0μM,4.0μMIncubationTime:24h,48hResult:IncreasedthelevelsofJC-1monmersandDCFH-DAfluorescenceintensity.体内研究KD36(30mg/kg,i.p.,oncedailyfor11days)significantlyinhibitstumorgrowthintheNCI-H358xenograftmicemodelswithatumorgrowthinhibition(TGI)rateof54.6%[1].AnimalModel:NCI-H358xenograftmicemodels(male,6weeks)[1]Dosage:30mg/kgAdministration:IntraperitoneallyinjectionResult:Reducedtumorweightandvolume.Showedtumorgrowthinhibition(TGI)rateof54.6%.Causednoobviouspathologicaldamagetomajororgans(heart,liver,spleen,lung,kidney),andexhibitednosystemictoxicity.REFERENCES[1].ShiJT,etal.Discoveryofnovelpyrimidine-basedKRAS-G12Cinhibitorswithpotentanti-NSCLCactivityviavirtualscreeningandstructureoptimization.EurJMedChem.2026;302(Pt3):118354.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.