ASCT2-IN-1-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEASCT2-IN-1Cat.No.:HY-163198分?式:C??H??Cl?N?O?分?量:627.56作?靶點:ASCT;mTOR;Apoptosis;Autophagy作?通路:PI3K/Akt/mTOR;Apoptosis;Autophagy儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性ASCT2-IN-1（compound20k）?種ASCT2抑制劑，在細胞A549和HEK293中的IC50值5.6μM和3.5μM。ASCT2-IN-1可以誘導細胞凋亡（apoptosis）。ASCT2-IN-1抑制腫瘤?長[1]。IC50&TargethumanASCT23.5μM(IC50)體外研究ASCT2-IN-1(50μM,15min)inhibitsGlnuptakeincellsA549andHEK293bytargetinghASCT2,withIC50valuesof5.6μMand3.5μM,respectively[1].ASCT2-IN-1(0-50μM,15min)improvedmetabolicstabilityinmurinelivermicrosome,withahalf-timeof37.15minandaclearanceof37.48μL/min?mg[1].ASCT2-IN-1(0-50μM,15min)inhibitsaminoacidtransporterSNAT2incellsA549aswellastransporterLAT1inoverexpressingHEK293[1].ASCT2-IN-1(5-10μM,24h)inhibitsGlnmetabolism,upregulatestheROSproductionandtherebyinducesapoptosisincellA549[1].ASCT2-IN-1(5-10μM,24h)inhibitsAKTphosphorylationandmTORC1activityunderstarvation,promotescellautophagy[1].ASCT2-IN-1(5-10μM,24h)dose-dependentlyinhibitsproliferationinA549[1].ASCT2-IN-1(0-10nM,96h)inhibitsorganoidproliferationofdrugresistantNSCLCsincellsH1975ORandHCC827OR[1].WesternBlotAnalysis[1]CellLine:A5491/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:5and10μMIncubationTime:24hResult:ActivatedCaspasereactionandinducedapoptosis.WesternBlotAnalysis[1]CellLine:A549Concentration:5and10μMIncubationTime:24hResult:DecreasedmTORC1andphosphorylarionofAKT.體內研究ASCT2-IN-2(i.p.;25or50mg/kg,onceeverytwodaysfor3weeks)inhibitstumorgrowthwithaTGIof65%inNSCLCxenograftmodelinBALB/cmice[1].PharmacokineticAnalysisofASCT2-IN-1inSprague-Dawleyrats[1]RouteDose(mg/kg)AUC0→t(μg?h/L)AUC0→∞(μg?h/L)T1/2(h)Tmax(h)Cmax(ng/mL)V/F(L/kg)CL/F(L/h/kg)MRT0→∞(h)Fr(%)i.p.10mg/kg2674.952824.429.411.17323.0749.543.6313.6977.04AnimalModel:NSCLCXenograftmodelinBALB/cnudemice[1]Dosage:25,50mg/kgAdministration:Intraperitonealinjection,onceeverytwodaysfor3weeksResult:InhibitedtumorgrowthwithTGIof65%.REFERENCES[1].QinL,etal.,DiscoveryofNovelAminobutanoicAcid-BasedASCT2InhibitorsfortheTreatmentofNon-Small-CellLungCancer.JMedChem.2024Jan13.doi:10.1021/acs.jmedchem.3c01093McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo