mTOR-inhibitor-8-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEmTORinhibitor-8Cat.No.:HY-131344CASNo.:2489196-70-3分⼦式:C₂₄H₁₉ClN₄OS分⼦量:446.95作⽤靶点:mTOR;Autophagy作⽤通路:PI3K/Akt/mTOR;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(55.93mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2374mL11.1869mL22.3739mL5mM0.4475mL2.2374mL4.4748mL10mM0.2237mL1.1187mL2.2374mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(4.65mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.65mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性mTORinhibitor-8⼀种mTOR抑制剂和⾃噬(autophagy)诱导剂。mTORinhibitor-8通过FKBP12抑制mTOR活性，并诱导A549⼈肺癌细胞⾃噬[1]。IC50&TargetmTORAutophagy体外研究mTORinhibitor-8(Compound5e;0.1-10ꢀμM;24and48hours)suppressesthegrowthofA549cellsinadose-dependentmanner[1].mTORinhibitor-8inducesautophagyinanmTOR-dependentmanner.mTORinhibitor-8(10ꢀμM;3-24ꢀhours)inducesautophagyinatime-dependentmanner.ThelevelsofLC3B-IIareenhanced[1].mTORinhibitor-8(10ꢀμM;3-24ꢀhours)reducesthephosphorylationofRPS6KB1(ribosomalproteinS6kinase)andEIF4EBP1(eukaryotictranslationinitiationfactor4E-bindingprotein1),twoessentialsubstratesofmTOR[1]CellViabilityAssay[1]CellLine:A549cellsConcentration:0.1,1,5,10ꢀμMIncubationTime:24and48hoursResult:SuppressedthegrowthofA549cellswithanIC50of2.6±0.11μM.WesternBlotAnalysis[1]CellLine:A549cellsConcentration:10ꢀμMIncubationTime:3,6,12and24ꢀhoursResult:ThelevelsofphosphorylationofRPS6KB1andEIF4EBP1weresignificantlydecreasedaftertreatment.体内研究mTORinhibitor-8(25and50μM;6days)effectivelyinhibitstumorgrowthinvivowithoutadverseeffectonnormalchickchorioallantoicmembraneangiogenesis[1].AnimalModel:Fertilechickeneggs(7-9daysold)[1]Dosage:25and50μM2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:6daysResult:SignificantxenografttumorremissionwasobservedineggscomparedwiththeDMSO-treatedeggs.REFERENCES[1].ZhaoMinLin,etal.Discoveryofnewfluorescentthiazole-pyrazolinederivativesasautophagyinducersbyinhibitingmTORactivityinA549humanlungcancercells.CellDeathDis.2020Jul20;11(7):551.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical