Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEmTORinhibitor-8Cat.No.:HY-131344CASNo.:2489196-70-3分?式:C??H??ClN?OS分?量:446.95作?靶點(diǎn):mTOR;Autophagy作?通路:PI3K/Akt/mTOR;Autophagy儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(55.93mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2374mL11.1869mL22.3739mL5mM0.4475mL2.2374mL4.4748mL10mM0.2237mL1.1187mL2.2374mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(4.65mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.65mM);ClearsolutionBIOLOGICALACTIVITY?物活性mTORinhibitor-8?種mTOR抑制劑和?噬(autophagy)誘導(dǎo)劑。mTORinhibitor-8通過FKBP12抑制mTOR活性，并誘導(dǎo)A549?肺癌細(xì)胞?噬[1]。IC50&TargetmTORAutophagy體外研究mTORinhibitor-8(Compound5e;0.1-10?μM;24and48hours)suppressesthegrowthofA549cellsinadose-dependentmanner[1].mTORinhibitor-8inducesautophagyinanmTOR-dependentmanner.mTORinhibitor-8(10?μM;3-24?hours)inducesautophagyinatime-dependentmanner.ThelevelsofLC3B-IIareenhanced[1].mTORinhibitor-8(10?μM;3-24?hours)reducesthephosphorylationofRPS6KB1(ribosomalproteinS6kinase)andEIF4EBP1(eukaryotictranslationinitiationfactor4E-bindingprotein1),twoessentialsubstratesofmTOR[1]CellViabilityAssay[1]CellLine:A549cellsConcentration:0.1,1,5,10?μMIncubationTime:24and48hoursResult:SuppressedthegrowthofA549cellswithanIC50of2.6±0.11μM.WesternBlotAnalysis[1]CellLine:A549cellsConcentration:10?μMIncubationTime:3,6,12and24?hoursResult:ThelevelsofphosphorylationofRPS6KB1andEIF4EBP1weresignificantlydecreasedaftertreatment.體內(nèi)研究mTORinhibitor-8(25and50μM;6days)effectivelyinhibitstumorgrowthinvivowithoutadverseeffectonnormalchickchorioallantoicmembraneangiogenesis[1].AnimalModel:Fertilechickeneggs(7-9daysold)[1]Dosage:25and50μM2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAdministration:6daysResult:SignificantxenografttumorremissionwasobservedineggscomparedwiththeDMSO-treatedeggs.REFERENCES[1].ZhaoMinLin,etal.Discoveryofnewfluorescentthiazole-pyrazolinederivativesasautophagyinducersbyinhibitingmTORactivityinA549humanlungcancercells.CellDeathDis.2020Jul20;11(7):551.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical