ASCT2-IN-1-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEASCT2-IN-1Cat.No.:HY-163198分⼦式:C₃₆H₃₂Cl₂N₂O₄分⼦量:627.56作⽤靶点:ASCT;mTOR;Apoptosis;Autophagy作⽤通路:PI3K/Akt/mTOR;Apoptosis;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性ASCT2-IN-1（compound20k）⼀种ASCT2抑制剂，在细胞A549和HEK293中的IC50值5.6μM和3.5μM。ASCT2-IN-1可以诱导细胞凋亡（apoptosis）。ASCT2-IN-1抑制肿瘤⽣长[1]。IC50&TargethumanASCT23.5μM(IC50)体外研究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—您⾝边的抑制剂⼤师www.MedChemEConcentration:5and10μMIncubationTime:24hResult:ActivatedCaspasereactionandinducedapoptosis.WesternBlotAnalysis[1]CellLine:A549Concentration:5and10μMIncubationTime:24hResult:DecreasedmTORC1andphosphorylarionofAKT.体内研究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