EP26-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEEP26Cat.No.:HY-159101分子式:C₄₂H₄₂ClFN₄O₅分子量:737.26作用靶点:EGFR;PD-1/PD-L1作用通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK;Immunology/Inflammation储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性EP26是一种有效的和具有口服活性的EGFR和PD-L1抑制剂，IC50值分别为48.6nM和1.77µM。EP26降低了p-EGFR的蛋白表达。EP26诱导细胞周期停滞在G0/G1期。EP26具有研究胶质母细胞瘤的潜力[1]。IC50&TargetEGFRPD-L148.6nM(IC50)1.77μM(IC50)体外研究EP26(0-4µM;48h)decreasestheproteinexpressionofp-EGFRinadose-dependentmanner[1].EP26(0.5,1,2µM;48h)inducescellcyclearrestatG0/G1phase[1].EP26bindsbindstohumanPD-L1andmurinePD-L1inadose-dependentmannerwithKDsof0.58,0.52µM,respectively[1].CellProliferationAssay[1]CellLine:U87MG,U251,U87MG-vIII,GL261cellsConcentration:0-20µMIncubationTime:72hResult:ShowedantiproliferativeactivitywithIC50sof0.77,1.02,1.19,0.28µMforU87MG,U251,U87MG-vIII,GL261cells,respectively.WesternBlotAnalysis[1]CellLine:U87MG,U87vIIIcells1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEConcentration:0,0.25,1,2µMforU87MGcells,0,0.5,1,2,4µMIncubationTime:48hResult:Decreasedtheproteinexpressionofp-EGFRinadose-dependentmanner.CellCytotoxicityAssay[1]CellLine:U87MGcellsConcentration:0.5,1,2µMIncubationTime:48hResult:InducedcellcyclearrestatG0/G1phasewiththepercentageofU87MGcellsinG0/G1phaseincreasedfrom60.51to63.57,69.48,and73.98%,respectively.体内研究EP26(50,100mg/kg;p.o.;onceadayfor21days)showsantitumoractivityinmice[1].PharmacokineticParametersinMaleSDrats[1].PKparametersi.v.administration(4mg/kg,n=5)p.o.administration(20mg/kg,n=5)AUC(0-t)(µg/L*h)2832.5±954.83145.7±778.7AUC(0-∞)(µg/L*h)2906.6±1061.83238.3±752.2MRT(0-t)(h)12.7±0.817.5±1.6MRT(0-∞)(h)2906.6±1061.83238.3±752.2t1/2(h)6.8±3.713.0±5.3Tmax(h)0.04±0.023.6±0.9Vz(L/kg)13.7±4.4123.5±64.6CL(L/h/kg)1.5±0.66.4±1.3Cmax(µg/L)325.6±166.8255.3±123.0F(%)-22.2AnimalModel:C57BL/6mice(GL261cells)[1]Dosage:50,100mg/kgAdministration:P.o.;onceadayfor21daysResult:Decreasedthetumorweightandtumorvolumeby92.0and89.7%at100mg/kg,significantlyinhibitedglioblastomatumorgrowthwithtumorgrowthinhibitions(TGIs)of61.4%,89.4%at50,100mg/kg,respectively.REFERENCESYangZ,etal.DiscoveryofNovelSmall-Molecule-BasedPotentialPD-L1/EGFRDualInhibitorswithHighDruggabilityforGlioblastomaImmunotherapy.JMedChem.2024May23;67(10):7995-8019.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica