BGT226-NVP-BGT226-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBGT226Cat.No.:HY-13334ACASNo.:915020-55-2Synonyms:NVP-BGT226分⼦式:C₂₈H₂₅F₃N₆O₂分⼦量:534.53作⽤靶点:PI3K;mTOR;Autophagy作⽤通路:PI3K/Akt/mTOR;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性BGT226(NVP-BGT226)⼀种PI3K(针对PI3Kα，PI3Kβ，PI3Kγ的IC50分别4nM，63nM，38nM)/mTOR双抑制剂，对⼈头颈癌细胞具有较强的⽣长抑制活性[1][2]。IC50&TargetPI3KαPI3KβPI3KγmTOR4nM(IC50)63nM(IC50)38nM(IC50)Autophagy体外研究BGT226showssignificantgrowthinhibitionorsignalblockageprofilescomparedwithLY294002andRapamycin.BGT226(10-10000nM)inhibitsFaDuandOECM1cellsgrowthwithIC50sof23.1±7.4and12.5±5.1nM,respectively[2].Theexpressionlevelsofp-mTORSer2481aredecreasedinBGT226-treatedcelllines(200nM;24hours)andbothp-AKTSer473andp-mTORSer2448arealsodecreasedinBGT226-treatedcelllines[2].CellViabilityAssay[2]CellLine:FaDucells;OECM1cellsConcentration:10,100,1000,10000nMIncubationTime:Result:InhibitedFaDuandOECM1cellsgrowthwithIC50sof23.1±7.4and12.5±5.1nM,1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemErespectively.WesternBlotAnalysis[2]CellLine:FaDucells;OECM1cellsConcentration:200nMIncubationTime:24hoursResult:p-mTORSer2481expressionlevelsdecreased,andbothp-AKTSer473andp-mTORSer2448expressionlevelsalsodecreased.体内研究BGT226(2.5and5mg/kg;oraladministrationfor21daysinmaleathymicmice)causes34.7%and76.1%reductionofthetumorgrowthonday21comparedwithcontrol[2].AnimalModel:Maleathymicmice(strainBALB/cAnN.Cg-Foxn1nu/CrlNarl)withFaDucellxenograftedmousemodel[2]Dosage:2.5and5mg/kgAdministration:Oraladministration;21daysResult:Caused34.7%and76.1%reductionofthetumorgrowth.户使⽤本产品发表的科研⽂献•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•FrontPharmacol.2020Nov11;11:580407.•Molecules.2020Apr23;25(8):1980.•HarvardMedicalSchoolLINCSLIBRARYSeemorecustomervalidationsonwww.MedChemEREFERENCES[1].MarkmanB,etal.PhaseIsafety,pharmacokinetic,andpharmacodynamicstudyoftheoralphosphatidylinositol-3-kinaseandmTORinhibitorBGT226inpatientswithadvancedsolidtumors.AnnOncol.2012Sep;23(9):2399-408.[2].ChangKY,etal.Novelphosphoinositide3-kinase/mTORdualinhibitor,NVP-BGT226,displayspotentgrowth-inhibitoryactivityagainsthumanheadandneckcancercellsinvitroandinvivo.ClinCancerRes.2011Nov15;17(22):7116-26.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications