Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIsorhamnetinCat.No.:HY-N0776CASNo.:480-19-3Synonyms:3'-Methylquercetin分?式:C??H??O?分?量:316.26作?靶點:MEK;PI3K;EndogenousMetabolite作?通路:MAPK/ERKPathway;PI3K/Akt/mTOR;MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:100mg/mL(316.20mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1620mL15.8098mL31.6196mL5mM0.6324mL3.1620mL6.3239mL10mM0.3162mL1.5810mL3.1620mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(6.58mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Isorhamnetin從中草藥沙棘(HippophaerhamnoidesL.)中提取的類酮化合物。Isorhamnetin可通過直接抑制MEK1和PI3K來抑制?膚癌。IC50&TargetMEK1PI3-KHumanEndogenousMetabolite體外研究Isorhamnetinisaplantflavonoidthatoccursinfruitsandmedicinalherbs.IsorhamnetinbindsdirectlytoMEK1inanATP-noncompetitivemannerandtoPI3-KinanATP-competitivemanner.InvitroandexvivokinaseassaydatashowthatIsorhamnetininhibitsthekinaseactivityofMAP/ERKkinase(MEK)1andPI3-KandtheinhibitionisduetodirectbindingwithIsorhamnetin[1].IsorhamnetininhibitstheAkt/mTORandMEK/ERKsignalingpathways,andpromotestheactivityofthemitochondrialapoptosissignalingpathway.TheinhibitoryeffectsofIsorhamnetinonbreastcancercellsaredeterminedusingtheCCK-8method.Isorhamnetininhibitstheproliferationofnumerousbreastcancercells(IC50,~10μM),includingMCF7,T47D,BT474,BT-549,MDA-MB-231andMDA-MB-468,whereaslessinhibitoryactivityisobservedintheMCF10Anormalbreastepithelialcellline(IC50,38μM)[2].體內研究PhotographicdatashowsthatIsorhamnetintreatmentsuppressestumordevelopmentinmice.Theaveragevolumeoftumorsinuntreatedmiceincreasesovertimeandreachesavolumeof623mm3at4weekspost-inoculation;however,atthistime,inmicetreatedwith1or5mg/kgIsorhamnetin,theaveragetumorvolumeisonly280or198mm3,respectively.Attheendofthestudy,Isorhamnetintreatment(1or5mg/kg)reducestumorweightcomparedwiththeuntreatedcontrolgroup[1].PROTOCOLCellAssay[2]MCF7,T47D,BT474,BT-549,MDA-MB-231andMDA-MB-468breastcancercelllines,aswellasaMCF10Anormalbreastepithelialcellline(control)areseededinto96-wellplatesatadensityof5×103cells/wellin100μLDMEMandplacedincellincubatorfor12hat37°Cinanatmospherecontaining5%CO2.ThecellsarethentreatedwithvariousconcentrationsofIsorhamnetin(100,33.3,11.1,3.7,1.2,0.4and0μM)for48h,andcellproliferationratesaredeterminedbyadding10μLCCK-8solutionpriortoincubationat37°Cfor2h.Theabsorbanceismeasuredatawavelengthof450nmusingaSpectraMax190MicroplateReader.Foreachassay,fourparallelwellsareincluded,andthehalfmaximalinhibitoryconcentration(IC50)ismeasuredusingtheinhibitioncurveandpresentedasthemeanofthreeindependentexperiments[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1]FemaleathymicnudemiceareinjectedsubcutaneouslyintheflankwithA431cells(1×106cellsin50μLofmediumand50μLofMatrigel).Cellsareallowedtoformtumors,andoncethetumorsreachasizeof402/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEmm3,themicearerandomlyassignedintogroups(6mice/group)andtreatedwith(1or5mg/kgbodyweight)orwithoutIsorhamnetinin40%DMSO/PBSbuffer,administeredintraperitoneallyeveryotherdayfor28days.Tumorsizeismeasuredeveryweekwithcalipers,andthetumorvolumeiscalculated.Micearesacrificedafter28daysoftreatmentwhenthecontroltumorsreachapproximately600mm3.Thetumorsareharvested,photographed,andweighed.Tumortissuesareusedforwesternblotanalysisandimmunohistochemicalanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發表的科研?獻?ActaPharmSinB.2021Jan;11(1):143-155.?FoodChem.2022:134807.?FrontCardiovascMed.2022;9:804801.?InvestOphthalmolVisSci.2021Mar1;62(3):38.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KimJE,etal.IsorhamnetinsuppressesskincancerthroughdirectinhibitionofMEK1andPI3-K.CancerPrevRes(Phila).2011Apr;4(4):582-91.[2].HuS,etal.IsorhamnetininhibitscellproliferationandinducesapoptosisinbreastcancerviaAktandmitogenactivatedproteinkinasekinasesignalingpa