Ipatasertib-tosylate-GDC-0068-tosylate-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIpatasertibtosylateCat.No.:HY-15186CCASNo.:1491138-24-9Synonyms:GDC-0068tosylate;RG7440tosylate分⼦式:C₃₁H₄₀ClN₅O₅S分⼦量:630.2作⽤靶点:Organoid;Akt;Apoptosis作⽤通路:StemCell/Wnt;PI3K/Akt/mTOR;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Ipatasertib(GDC-0068)tosylate⼀种⼝服有效的、⾼选择性和ATP竞争性泛Akt抑制剂，其对Akt1/2/3的IC50值分别为5、18、8nM。Ipatasertib通过抑制Akt导致⾮p53依赖性的PUMA激活，从⽽同步激活FoxO3a和NF-κB。Ipatasertib还能诱导癌细胞凋亡(apoptosis)，抑制异种移植⼩⿏模型中的肿瘤⽣长。IC50&TargetAkt1Akt2Akt3PKA5nM(IC50)18nM(IC50)8nM(IC50)3100nM(IC50)体外研究Ipatasertibtosylate(10µM;12,24h)suppressescoloncancercellproliferationbyp53irrespectivelyactivatingPUMAinvitro[1].Ipatasertibtosylate(1,5,10,20μM;24h/10μM;3,6,12,24h)up-regulatestheexpressionlevelofPUMAinaconcentrationandtimedependentmannerinHCT116cells[1].IpatasertibtosylateincreasesthemRNAlevelofPUMAinHCT116WT,p53−/−,andDLD1(p53mutant)cells[1].Ipatasertibtosylate(10µM;24h)inducesapoptosisthroughPUMA/BaxpathwayinHCT116cells[1].CellViabilityAssay[1]CellLine:HCT116WT,p53−/−,andDLD1(p53mutant)cellsConcentration:10µMIncubationTime:12,24h1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Decreasedallthethreecelllinesviability.ApoptosisAnalysis[1]CellLine:HCT116cellsConcentration:10µMIncubationTime:24hResult:InducedapoptosisthroughPUMA/Baxpathway.WesternBlotAnalysis[1]CellLine:HCT116WT,p53−/−,andDLD1(p53mutant)cellsConcentration:1,5,10,20μMfor24h/10μMfor3,6,12,24hIncubationTime:24h;3,6,12,24hResult:IncreasedthelevelofPUMAinaconcentrationandtimedependentmanner.体内研究Ipatasertibtosylate(30mg/kg;p.o.;singledailyfor15consecutivedays)exhibitsPUMA-dependentantitumoractivityinHCT116WTandPUMA−/−cellsxenograftnudemicemodel[1].AnimalModel:HCT116WTandPUMA−/−cellsxenograftnudemicemodel[1].Dosage:30mg/kgAdministration:Oralgavage;singledailyfor15consecutivedays.Result:InhibitedgrowthoftumorsinaPUMA-dependentmanner.户使⽤本产品发表的科研⽂献•CellMetab.2021Nov2;33(11):2247-2259.e6.•Blood.2023May26;blood.2022018752.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•MolCell.2020Sep17;79(6):1008-1023.e4.•MolCell.2019Jan3;73(1):22-35.e6.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].SunL,etal.Ipatasertib,anovelAktinhibitor,inducestranscriptionfactorFoxO3aandNF-κBdirectlyregulatesPUMA-dependentapoptosis.CellDeathDis.2018Sep5;9(9):911.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap