Doxifluridine-d3-Ro-21-9738-d-sub-3-sub-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEDoxifluridine-d3Cat.No.: HY-B0021S1Synonyms: Ro21-9738-d3;5-Fluoro-5'-deoxyuridine-d3;5'-DFUR-d3分子式: C₉H₈D₃FN₂O₅分子量: 249.21作用靶点: ThymidylateSynthase;Isotope-LabeledCompounds作用通路: Apoptosis;Others储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Doxifluridine-d3是氘代标记的Doxifluridine(HY-B0021)。Doxifluridine具有抗癌活性。Doxifluidine是一种5-FU前药。Doxifluridine是胸腺嘧啶酸合酶抑制剂。Doxifluridine能通过协同多种药物增强对肿瘤的抑制[1][2][3]。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].Doxifluridine(1-10μM)inhibitsangiogenesisbysignificantlyinhibitingtheexpressionofVEGFinFU-MMT-1cells[2].Doxifluridine(1-100μM)slightlyincreasestheexpressionofTSP-1atlowdose(1μM)andinhibitstheexpressionofTSP-1athighdose(100μM)inFU-MMT-1cells[2].Doxifluridine(100μM)inhibitscellproliferationinHUVECcells[2].体内研究Doxifluridine(61.55mg/kg;Intragastricadministration;Singledose)hasanticanceractivityinBALB?cAJcl-numice,andcansignificantlyenhanceanticanceractivityincombinationwithTNP-470(HY-101932)[2].Doxifluridine(200mg/kg;Intraperitonealinjection;Singledose)caninhibitthymidinesynthaseactivityinDMH-inducedcoloncancermice[3].REFERENCESNaganumaY,etal.Metronomicdoxifluridinechemotherapycombinedwiththeanti-angiogenicagentTNP-470inhibitsthegrowthofhumanuterinecarcinosarcomaxenografts.CancerSci.2011Aug;102(8):1545-52.1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEBerneM,etal.Inhibitionofthymidylatesynthaseafteradministrationofdoxifluridineinatransplantablecoloncarcinomaintherat.CancerInvest.1988;6(4):377-83.DiBartolomeoM,etal.Integratedtreatmentwithdoxifluridineandradiotherapyinrecurrentorprimaryunresectablerectalcancer.Afeasibilitystudy.Tumori.1999May-Jun;85(3):211-3.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear