KTC1101-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEKTC1101Cat.No.:HY-162382CASNo.:2764833-47-6分子式:C₂₁H₂₆F₂N₈O₃分子量:476.48作用靶点:PI3K;Akt;mTOR作用通路:PI3K/Akt/mTOR储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性KTC1101是一种口服活性的泛PI3K抑制剂。KTC1101可抑制PI3K信号通路，并减少下游AKT和mTOR磷酸化，降低Ki67的表达量。KTC1101的抗肿瘤活性有双重作用机制，即直接抑制肿瘤细胞生长和动态增强免疫反应[1]。IC50&TargetKi67PI3KαPI3KβPI3Kδ3.72nM(IC50)36.29nM(IC50)1.22nM(IC50)PI3KγPI3K17.09nM(IC50)体外研究KTC1101(0.1-50000nM,48h)candose-dependentlyinducecellcyclestagnationinG1phaseinalltestedcelllines(PC3,TMD8,HSC2,HSC4,andCAL33cells).KTC1101hasanti-proliferativeactivity,withtheIC50rangingfrom20nMto130nM,buthasnosignificantpromotionofapoptosis[1].KTC1101(0.1-1000nM,1h)exhibitssignificantinhibitoryactivityagainstallPI3KisoformsintheAdaptakinaseassay.TheIC50valuesofKTC1101forPI3Kα,PI3Kβ,PI3KδandPI3Kγare3.72nM,36.29nM,1.22nMand17.09nMrespectively[1].KTC1101(0-125nM,48h)effectivelyinhibitsthePI3KsignalingpathwayinWBexperiments,reducesthephosphorylationofPI3KdownstreameffectorsAKTandmTOR[1].CellViabilityAssay[1]CellLine:39humantumorcelllines,PC3,TMD8,HSC2,HSC4,CAL33cells,etc.Concentration:0.1,1,10,100,1000,25000,50000nM1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEIncubationTime:48hResult:ExhibitedanaverageGI50valueof23.4nMacrossallcelllinestested,significantlylowerthanZSTK474(HY-50847)(320nM)andCopanlisib(HY-15346)(134nM).WesternBlotAnalysis[1]CellLine:PC3cells,TMD8cellsConcentration:0,5,25,125nMIncubationTime:48hResult:ShowedbetterinhibitoryperformanceinTMD8cellscomparedwithZSTK474(HY-50847)andCopanlisib(HY-15346).体内研究KTC1101(0-125mg/kg/dayfor14days,p.o.)canarresttumorgrowthinmicewithhumantumorxenograftsandshownosignsofrecurrence[1].PharmacokineticAnalysisintumorxenograftmousemodel[1]RouteDose(mg/kg)t1/2(h)Tmax(h)Cmax(μg/mL)AUC0-t(μg/mL*h)Vz/F>(L/kg)CLz/F(L/h/kg)p.o.1007.190.671.669.33117.9610.71REFERENCESPengX,etal.Anovelpan-PI3KinhibitorKTC1101synergizeswithanti-PD-1therapybytargetingtumorsuppressionandimmuneactivation.MolCancer.2024Mar14;23(1):54.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear