Ipatasertib-tosylate-GDC-0068-tosylate-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIpatasertibtosylateCat.No.:HY-15186CCASNo.:1491138-24-9Synonyms:GDC-0068tosylate;RG7440tosylate分?式:C??H??ClN?O?S分?量:630.2作?靶點:Organoid;Akt;Apoptosis作?通路:StemCell/Wnt;PI3K/Akt/mTOR;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Ipatasertib(GDC-0068)tosylate?種?服有效的、?選擇性和ATP競爭性泛Akt抑制劑，其對Akt1/2/3的IC50值分別為5、18、8nM。Ipatasertib通過抑制Akt導致?p53依賴性的PUMA激活，從?同步激活FoxO3a和NF-κB。Ipatasertib還能誘導癌細胞凋亡(apoptosis)，抑制異種移植??模型中的腫瘤?長。IC50&TargetAkt1Akt2Akt3PKA5nM(IC50)18nM(IC50)8nM(IC50)3100nM(IC50)體外研究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?邊的抑制劑?師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.體內研究Ipatasertibtosylate(30mg/kg;p.o.;singledailyfor15consecutivedays)exhibitsPUMA-dependentantitumoractivityinHCT116WTandPUMA?/?cellsxenograftnudemicemodel[1].AnimalModel:HCT116WTandPUMA?/?cellsxenograftnudemicemodel[1].Dosage:30mg/kgAdministration:Oralgavage;singledailyfor15consecutivedays.Result:InhibitedgrowthoftumorsinaPUMA-dependentmanner.戶使?本產品發(fā)表的科研?獻?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?邊的抑制劑?師www.MedChemE[1].SunL,etal.Ipatasertib,anovelAktinhibitor,inducestranscriptionfactorFoxO3aandNF-κBdirectlyregulatesPUMA-dependentapoptosis.CellDeathDis.2018Sep5;9(9):911.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap