Didox-NSC-324360-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDidoxCat.No.:HY-19387CASNo.:69839-83-4Synonyms:NSC-324360分⼦式:C₇H₇NO₄分⼦量:169.13作⽤靶点:DNA/RNASynthesis作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(591.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM5.9126mL29.5631mL59.1261mL5mM1.1825mL5.9126mL11.8252mL10mM0.5913mL2.9563mL5.9126mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.75mg/mL(16.26mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(16.26mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(16.26mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Didox(NSC-324360)⼀种合成的核糖核苷酸还原酶(ribonucleotidereductase,RR)抑制剂。IC50&TargetRibonucleotidereductase[1]体外研究Didox(NSC-324360)suppressesLPS-inducedmRNAlevelsofiNOS,IL-6,IL-1,TNF-α,NF-κβ(p65),andp38-α,after24hoftreatment.TreatmentwithDidoxalsosuppressesthesecretionofnitricoxide(NO),IL-6,andIL-10.Usingmitochondrialdehydrogenaseactivityasameasureofcytotoxicity,theeffectsofDidoxoncellularrespirationinRAW264.7areexaminedoverarangeofconcentrationsfor24h.Cellsexposuresto200μMandbelowDidox,withandwithoutLPS,donotexhibitsignificantcellulartoxicity[1].Didox(NSC-324360)isactiveagainstallhumanandmurineacutemyeloidleukemia(AML)linestestedwithIC50valuesinthelowmicromolarrange(meanIC5037µM[range25.89-52.70µM])[2].体内研究Onceengraftmentisestablishedbybioluminescentimaging,theanimalsreceivedailyadministrationsofDidoxat425mg/kgviaIPinjectionover5days.Didox(NSC-324360)treatmentsignificantlyreducesleukemicburdencomparedtovehicletreatedcontrols(p=0.0026andp=0.0342).Moreimportantly,Didox(NSC-324360)providesasignificantsurvivalbenefit(p[2].PROTOCOLCellAssay[1]RAW264.7macrophagesaretreatedwithDidoxalone,with0.1μg/mLLPS,orthetwoincombination.Cellularrespiration,asanindicationofcytotoxicity,ismeasuredbytheMTTassay,whichquantifiesmitochondrialdehydrogenaseactivity.Macrophagesareplatedinto96wellCostarplatesat105cellsperwellin100μLofDMEMmedia.After4hofincubationat37°Cforadherence,compoundsandDMSOcarriercontrol(0.01%final)areaddedintriplicateoverserialdilutionsbeginningwith200μMperwellinatotalvolumeof200μL,andtheplatesincubatedfor24h.Fourhbeforeterminationoftheassay,eachwellreceives20μLofa5mg/mLMTTsolutioninun-supplementedDMEM.Aftercentrifugation,thesupernatantforeachwellisdiscardedandcellscontainingreducedMTTaresolubilizedwith100μLofacidifiedisopropanol(4mMHCl,0.1%NP-40inisopropanol).Followingabriefperiodofshaking,theopticaldensity(O.D.)foreachwellisrecordedat550nm.Eachexperimentisrepeatedthreetimesandthedataaveragedfromeachtriplicate,thenexpressedaspercentageofthecontrolO.D.valuesforeachexperiment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[2]Administration[2]Luciferase-taggedleukemiacellsaretransplantedinto8-weekold,sublethallyirradiated(4.5Gy)C57Bl/62/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEmicebytailveininjectionof1.0×106cellspermouse.Miceareinjectedwith150mg/kgD-Luciferin,anesthetisedwithIsoflurane,andimagedusingtheIVIS100imagingsystem.MicebegintreatmentwithDidoxupondetectionofclearsignal.TheanimalsaretreatedwithdailyadministrationsofDidox(NSC-324360)at425mg/kgDidoxbyintraperitonealinjection(IP)for5days.Controlanimalsreceive5%dextrosewaterbyIPinjection.Repeatimagingisperformedonthedayfollowingthefinaltreatment[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•FreeRadicBiolMed.2020May20;152:525-539.•OxidMedCellLongev.2018Mar20;2018:7616852.•PhytotherRes.2022Feb7.•Biomolecules.2022Feb12;12(2):299.•JEthnopharmacol.2021Sep30;114694.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MatsebatlelaTM,etal.3,4-Dihydroxy-benzohydroxamicacid(Didox)suppressespro-inflammatoryprofilesandoxidativestressinTLR4-activatedRAW264.7murinemacrophages.ChemBiolInteract.2015May25;233:95-105.[2].CookGJ,etal.TheefficacyoftheribonucleotidereductaseinhibitorDidoxinpreclinicalmodel