Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemE5-FluorouracilCat.No.:HY-90006CASNo.:51-21-8分?式:C?H?FN?O?分?量:130.08作?靶點:NucleosideAntimetabolite/Analog;HIV;Apoptosis;EndogenousMetabolite作?通路:CellCycle/DNADamage;Anti-infection;Apoptosis;MetabolicEnzyme/Protease儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfromlight)溶解性數(shù)據(jù)體外實驗H2O:20mg/mL(153.75mM;Needultrasonic)掃描?維碼，DMSO:15mg/mL(115.31mM;Needultrasonicand運?溶解?案計算器warming)獲得適合您實驗體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM7.6876mL38.4379mL76.8758mL5mM1.5375mL7.6876mL15.3752mL10mM0.7688mL3.8438mL7.6876mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶1.請依序添加每種溶劑：5%DMSO40%PEG3005%Tween-8050%saline2.Solubility:≥2.5mg/mL(19.22mM);Clearsolution請依序添加每種溶劑：5%DMSO95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(19.22mM);Clearsolution1/3www.MedChemEwww.MedChemEBIOLOGICALACTIVITY?物活性5-Fluorouracil(5-FU)?種尿嘧啶的類似物(nucleosideantimetabolite/analog)，?種有效的抗腫瘤藥。5-Fluorouracil通過抑制胸苷酸合成酶響嘧啶的合成，從?耗盡細胞內(nèi)dTTP池。5-Fluorouracil誘導(dǎo)細胞凋亡(apoptosis)，可?作化學敏化劑。5-Fluorouracil還可抑制HIV病毒。5-Fluorouracil(5-FU)可破壞外泌體特異性的rRNA。IC50&TargetHIVHumanEndogenousMetabolite體外研究5-Fluorouracil(5-Fu)andNSC123127(Dox)showsynergisticanticancerefficacy.TheIC50valueof5-Fu/Dox-DNMtowardhumanbreastcancer(MDA-MB-231)cellsis0.25μg/mL,presentingan11.2-foldand6.1-foldincreaseincytotoxicitycomparedtoDox-DNMand5-Fu-DNM,respectively[1].In5-fluorouracil(5-FU)andCDDPtreatedNFBD1-inhibitedNPCcells,theNFBD1expressioninNPCCNE1celllinesisdepletedusinglentivirus-mediatedshorthairpinRNA,andthesensitivityofthesecellsiselevated.NFBD1knockdownleadstoanobviousinductionofapoptosisinCDDP-or5-FU-treatedCNE1cells[2].體內(nèi)研究5-Fluorouracil(23mg/kg,3times/week)for14days,inducesacceleratedgastrointestinaltransitassociatedwithacuteintestinalinflammationatday3afterthestartoftreatment,whichmayhaveledtopersistentchangesintheENSobservedafterdays7and14oftreatmentcontributingtodelayedgastrointestinaltransitandcolonicdysmotility[4].PROTOCOLAnimalMicereceiveintraperitonealinjectionsof5-FU(23mg/kg),3timesaweekviaa26gaugeneedle.5-FUisAdministration[2]dissolvedin100%dimethylsulfoxide(DMSO)tomake1M/Lstocksolutionrefrigeratedat?20°C.Thestockisthendefrostedanddilutedwithsterilewatertomake0.1M/L(10%DMSO)solutionsforintraperitonealinjections.Thedoseof5-FUiscalculatedtobeequivalenttostandardhumandoseperbodysurfacearea.Thelowdosesof5-FU(10-40mg/kg)havebeenshowntohaveantitumorefficacyinmousemodelsofcancer.Sham-treatedmicereceived10%DMSOinsterilewaterviaintraperitonealinjectionthreetimesaweekviaa26gaugeneedle.Theinjectedvolumesarecalculatedtothebodyweight;themaximumvolumedoesnotexceed200μLperinjection.Miceareeuthanizedviacervicaldislocationat3(2treatments),7(3treatments),and14(6treatments)daysafterthefirstinjectionandcoloniscollectedforinvitroexperiments.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?CancerRes.2018Oct1;78(19):5586-5599.?Theranostics.2020Jan1;10(1):300-311.?Theranostics.2019Jul9;9(17):4878-4892.?JExpClinCancerRes.2019Aug14;38(1):353.?AnalChem.2016Apr5;88(7):3817-25.Seemorecustomervalidationsonwww.MedChemE2/3www.MedChemEwww.MedChemEREFERENCES[1].HanR,etal.Amphiphilicdendriticnanomicelle-mediatedco-deliveryof5-fluorouracilandNSC123127forenhancedtherapeuticefficacy.JDrugTarget.2016Jun29:1-28.[Epubaheadofprint][2].McQuadeRM,etal.Gastrointestinaldysfunctionandentericneurotoxicityfollowingtreatmentwithanticancerchemotherapeuticagent5-fluorouracil.NeurogastroenterolMotil.2016Jun28.[3].ZengQ,etal.KnockdownofNFBD1/MDC1enhanceschemosensitivitytoNSC119875or5-fluorouracilinnasopharyngealcarcinomaCNE1cells.MolCellBiochem.2016Jul;418(1-2):137-46.[4].YinL,etal.Antitumoreffectsofoncolyticherpessimplexvirustype2againstcolorectalcancerinvitroandinvivo.TherClinRiskManag.2017Feb7;13:117-130.[5].JonesDH,etal.Ten-YearandBeyondFollow-upAfterTreatmentWithHighlyPurifiedLiquid-InjectableSiliconeforHIV-AssociatedFacialLipoatrophy:AReportof164Patients.DermatolSurg.2019Jul;45(7):941-948.[6].SnyderSM,etal.InitialExperiencewithTopicalFluorouracilforTreatmentofHIV-AssociatedAnalIntraepithelialNeoplasia.JIntAssocPhysiciansAIDSCare(Chic).2011;10(2):83-88.[7].PekYeeLum,etal.Discoveringmodesofactionfortherapeuticcompoundsusingagenome-widescreenofyeastheterozygotes.Cell.2004Jan9;116(1):121-37.McePdfHeight關(guān)注M