Elaiophylin-Azalomycin-B-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEElaiophylinCat.No.:HY-15184CASNo.:37318-06-2Synonyms:AzalomycinB;Gopalamicin;EfomycinE分?式:C??H??O??分?量:1025.27作?靶點(diǎn):Autophagy;Antibiotic作?通路:Autophagy;Anti-infection儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(48.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.9754mL4.8768mL9.7535mL5mM0.1951mL0.9754mL1.9507mL10mM0.0975mL0.4877mL0.9754mL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:2.5mg/mL(2.44mM);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%cornoilSolubility:≥2.5mg/mL(2.44mM);ClearsolutionBIOLOGICALACTIVITY?物活性Elaiophylin(AzalomycinB;Gopalamicin;EfomycinE)?種?噬(autophagy)抑制劑，在巢癌細(xì)胞中作為單?藥劑發(fā)揮抗腫瘤活性[1]。IC50&TargetAutophagy[1]體外研究Elaiophylin-mediatedautophagyinhibitionandlysosomaldysfunctionaffectovariancancercellsurvivalduringhypoxia.ExposuretoElaiophylin(0.025-0.5μM;24hours)causesasignificantincreaseinovariancancerSKOV3celldeathinhypoxiaconditions[1].InboththeSKOV3andA2780celllines,Elaiophylin(0.25,0.5,0.75μM;24hours)treatmentleadstosignificantactivationofcleavedCASP9/caspase-9andPARP1anddownregulationofBIRC5/survivininaconcentration-dependentmanner[1].CellViabilityAssay[1]CellLine:OvariancancerSKOV3cells.Concentration:0.025,0.05,0.1,0.2,0.5μMIncubationTime:24hoursResult:CausedasignificantincreaseinovariancancerSKOV3cellsdeathinhypoxiaconditions.WesternBlotAnalysis[1]CellLine:OvariancancerSKOV3cells;A2780cellsConcentration:0.25,0.5,0.75μMIncubationTime:24hoursResult:TreatmentledtosignificantactivationofcleavedCASP9/caspase-9andPARP1anddownregulationofBIRC5/survivininaconcentration-dependentmanner.體內(nèi)研究Treatmentwith2mg/kgElaiophylin(giveni.p.every2daysfor21days;inBALB/Cathymicmice)significantlysuppressesovariancancerSKOV3cellsgrowthcomparedwithDMSOtreatment,resultingina72%decreaseintheaveragedailytumorgrowthratecomparedwithDMSOtreatment[1].LowerdosesofElaiophylinasasingleagentexertsignificantantitumoractivity,whilehigherdosesleadtointestinaltoxicity.Administrationofalowerdose(2mg/kg)ofElaiophylinasasingleagentachievesasignificantantitumoreffectwithouttoxicityinanorthotopicovariancancermodelwithmetastasis.Toxicreactionsareobservedonlyinthe8mg/kggroup[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:4-wk-oldBALB/CathymicmicewithovariancancerSKOV3cells[1]Dosage:1or2mg/kgAdministration:Giveni.p.every2daysfor21daysResult:Treatmentwith2mg/kgsignificantlysuppressedovariancancerSKOV3cellsgrowthcomparedwithDMSOtreatment.REFERENCES[1].ZhaoX,etalElaiophylin,anovelautophagyinhibitor,exertsantitumoractivityasasingleagentinovariancancercells.Autophagy.2015;11(10):1849-63.McePdfHeightCaution:Producthasnotb