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Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDaunorubicincitrateCat.No.:HY-108876CASNo.:1884557-85-0Synonyms:Daunomycin(citrate);RP13057(citrate);Rubidomycin(citrate)分?式:C??H??NO??分?量:719.64作?靶點:Topoisomerase;DNA/RNASynthesis;ADCCytotoxin;Autophagy;Bacterial;Antibiotic;Apoptosis作?通路:CellCycle/DNADamage;Antibody-drugConjugate/ADCRelated;Autophagy;Anti-infection;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Daunorubicin(Daunomycin)citrate?種拓撲異構酶II(topoisomeraseII)抑制劑,具有有效的抗腫瘤活性。Daunorubicincitrate抑制DNA和RNA合成(DNAandRNAsynthesis)。Daunorubicincitrate?種細胞毒素,可抑制癌細胞活?并誘導細胞凋亡(apoptosis)和壞死(necrosis)。Daunorubicincitrate還?種蒽環(huán)類抗?素。Daunorubicincitrate可?于研究感染和多種癌癥,包括??病、?霍奇?淋巴瘤、尤???瘤、維爾姆斯?瘤。IC50&TargetTopoisomeraseIIDaunorubicins/Doxorubicins體外研究Daunorubicincitrate(0-256μg/mL,30min)inhibitsDNAandRNAsynthesisinsensitiveandresistantEhrlichascitestumorcells[2].Daunorubicincitrate(7nM-1.9μM,72h)showschemosensitivityinMolt-4cellsandL3.6cells[3][4].Daunorubicincitrate(0.4μM,48h)inducesapoptoticandnecrosisinL3.6cells[4].Daunorubicincitrate(0.4μM,120min)inducesROSgenerationinL3.6cells[4].Daunorubicincitrate(2μM,24h)inducesautophagyinK562cells(myeloidcellline)[6].CellViabilityAssay[3][4]CellLine:Molt-4cells(ahumanT-lymphoblasticleukemiacellline),L3.6cells(metastatichumanpancreaticcellline)Concentration:7nM-1.9μM1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:72hResult:InhibitedcellviabilitywithIC50valuesof40nM(Molt-4)and400nM(L3.6).ApoptosisAnalysis[4]CellLine:L3.6cellsConcentration:0.4μMIncubationTime:24h,48hResult:Inducednecrosiswithoutapoptosisat24h,inducedbothanapoptoticandextensivenecroticresponseat48h.WesternBlotAnalysis[6]CellLine:K562cellsConcentration:2μMIncubationTime:24hResult:EnabledtheswitchofLC3-IintoLC3-II,accompaniedwithasignificantincreasedexpressionlevelofLC3.體內研究Daunorubicincitrate(intravenousinjection,3mg/kg,threetimesat48hintervals)producescardiotoxicityandnephrotoxicityinrats[5].Daunorubicincitrate(intraperitonealinjection,10mg/kg)inducessisterchromatidexchangesinmice[7].AnimalModel:MaleSprague-Dawleyrats[5]Dosage:3mg/kgAdministration:Intravenousinjection,threetimesat48hintervals.Result:CausedasignificantincreaseinMDA(malondialdehyde)levelinrenaltissue,accompaniedbyasignificantreductionintotalGPxactivity.Increasedurinaryproteinexcretion,serumcreatinine,andBUNlevel.戶使?本產品發(fā)表的科研?獻?ClinCancerRes.2020Apr15;26(8):2011-2021.?JControlRelease.2022Apr22;346:136-147.?JTranslMed.2022Jul6;20(1):304.?CellOncol.2022Aug29.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?Cancers(Basel).2021,13(5),1127.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LehmannM,etal.Activityoftopoisomeraseinhibitorsdaunorubicin,idarubicin,andaclarubicinintheDrosophilaSomaticMutationandRecombinationTest.EnvironMolMutagen.2004;43(4):250-7.[2].DanoK,etal.InhibitionofDNAandRNAsynthesisbydaunorubicininsensitiveandresistantEhrlichascitestumorcellsinvitro.CancerRes.1972Jun;32(6):1307-14.[3].SvenssonSP,etal.MelanininhibitscytotoxiceffectsofDoxorubicinandDaunorubicininMOLT4cells.PigmentCellRes.2003Aug;16(4):351-4.[4].GervasoniJEJr,etal.AneffectiveinvitroantitumorresponseagainsthumanpancreaticcarcinomawithpaclitaxelandDaunorubicinbyinductionofbothnecrosisandapoptosis.AnticancerRes.2004Sep-Oct;24(5A):2617-26.h[5].ArozalW,etal.TelmisartanpreventstheprogressionofrenalinjuryindaunorubicinratswiththealterationofangiotensinIIandendothelin-1receptorexpressionassociatedwithitsPPAR-γagonistactions.Toxicology.2011Jan11;279(1-3):91-9.[6].EmelineBollaert,etal.MiR-15a-5pConfersChemoresistanceinAcuteMyeloidLeukemiabyInhibitingAutophagyInducedbyDaunorubicin.IntJMolSci.2021May13;22(10):5153.[7].ChengWu,etal.DoxorubicinsuppresseschondrocytedifferentiationbystimulatingROSproduction.EurJPharmSci.2021Dec1;16

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