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MedKoo Biosciences/BIIB021/200505/50mg
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BIIB021,alsoknownasCNF2024,isanorallyactive,purine-scaffold,small-moleculeinhibitorofheatshockprotein90(HSP90)withpotentialantineoplasticactivity.HSP90inhibitorCNF2024specificallyblocksactiveHSP90,inhibitingitschaperonefunctionandpromotingthedegradationofoncogenicsignalingproteinsinvolvedintumorcellproliferationandsurvival;thismayresultintheinhibitionofcellularproliferationinsusceptIBLetumorcellpopulations.MedKooCat#:200505Name:BIIB021CAS#:848695-25-0(freebase)ChemicalFormula:C14H15ClN6OExactMass:318.09959MolecularWeight:318.76ElementalAnalysis:C,52.75;H,4.74;Cl,11.12;N,26.36;O,5.02RelatedCAS#:1225041-97-3(BIIB-021mesylate) Synonym:BIIB021;BIIB021;BIIB-021;CNF-2024;CNF2024;CNF2024.IUPAC/ChemicalName:[6-Chloro-9-(4-methoxy-3,5-dimethylpyridin-2-ylmethyl)-9H-purin-2-yl]amineInChiKey:QULDDKSCVCJTPV-UHFFFAOYSA-NInChiCode:InChI=1S/C14H15ClN6O/c1-7-4-17-9(8(2)11(7)22-3)5-21-6-18-10-12(15)19-14(16)20-13(10)21/h4,6H,5H2,1-3H3,(H2,16,19,20)SMILESCode:NC1=NC(Cl)=C2N=CN(CC3=NC=C(C)C(OC)=C3C)C2=N1TechnicalDataAppearance:SolidpowderPurity:>98%(orrefertotheCertificateofAnalysis)CertificateofAnalysis:ViewCoA:currentbatch,Lot#BBC60815QCData:ViewQCdata:currentbatch,Lot#BBC60815SafetyDataSheet(MSDS):ViewMaterialSafetyDataSheet(MSDS)ShippingCondition:Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.StorageCondition:Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).Solubility:SolubleinDMSO,notinwaterShelfLife:>5yearsifstoredproperlyDrugFormulation:ThisdrugmaybeformulatedinDMSOStockSolutionStorage:0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).HarmonizedSystemCode:293490AdditionalInformationBIIB021isanovel,fullysyntheticinhibitorofHsp90thatbindscompetitivelywithgeldanamycinintheATP-bindingpocketofHsp90.Intumorcells,BIIB021inducedthedegradationofHsp90clientproteinsincludingHER-2,AKT,andRaf-1andup-regulatedexpressionoftheheatshockproteinsHsp70andHsp27.BIIB021treatmentresultedingrowthinhibitionandcelldeathincelllinesfromavarietyoftumortypesatnanomolarconcentrations.OraladmiNISTrationofBIIB021ledtothedegradationofHsp90clientproteinsmeasuredintumortissueandresultedintheinhibitionoftumorgrowthinseveralhumantumorxenograftmodels.StudiestoinvestigatetheantitumoreffectsofBIIB021showedactivityonbothdailyandintermittentdosingschedules,providingdosescheduleflexibilityforclinicalstudies.AssaysmeasuringtheHER-2proteinintumortissueandtheHER-2extracellulardomaininplasmawereusedtoshowinterdictionoftheHsp90pathwayandutilityaspotentialbioMarkersinclinicaltrialsforBIIB021.Together,thesedatashowthatBIIB021isapromisingneworalinhibitorofHsp90withantitumoractivityinpreclinicalmodels.(source:MolCancerTher.2009Apr;8(4):921-9.).(source:MolCancerTher.2009Apr;8(4):921-9.).References1:XuL,WoodwardC,KhanS,PrakashC.InVitroMetabolismof6-Chloro-9-(4-methoxy-3,5-dimethylpyridin-2-ylmethyl)-9H-purin-2-ylamine(BIIB021),anInhibitorofHSP90,inLiverMicrosomesandHepatocytesofRats,Dogs,andHumansandRecombinantHumanCytochromeP450Isoforms.DrugMetabDispos.2012Jan4.[Epubaheadofprint]PubMedPMID:22217465.2:ZhangH,NeelyL,LundgrenK,YangYC,LoughR,TimpleN,BurrowsF.BIIB021,asyntheticHsp90inhibitor,hasbroadapplicationagainsttumorswithacquiredmultidrugresistance.IntJCancer.2010Mar1;126(5):1226-34.PubMedPMID:19676042.3:BöllB,EltaibF,ReinersKS,vonTresckowB,TawadrosS,SimhadriVR,BurrowsFJ,LundgrenK,HansenHP,EngertA,vonStrandmannEP.Heatshockprotein90inhibitorBIIB021(CNF2024)depletesNF-kappaBandsensitizesHodgkin'slymphomacellsfornaturalkillercell-mediatedcytotoxicity.ClinCancerRes.2009Aug15;15(16):5108-16.Epub2009Aug11.PubMedPMID:19671844.4:YinX,ZhangH,LundgrenK,WilsonL,BurrowsF,ShoresCG.BIIB021,anovelHsp90inhibitor,sensitizesheadandnecksquamouscellcarcinomatorADIotherapy.IntJCancer.2010Mar1;126(5):1216-25.PubMedPMID:19662650.5:LundgrenK,ZhangH,BrekkenJ,HuserN,PowellRE,TimpleN,BuschDJ,NeelyL,SensintaffarJL,YangYC,McKenzieA,FriedmanJ,ScannevinR,KamalA,HongK,KasibhatlaSR,BoehmMF,BurrowsFJ.BIIB021,anorallyavailable,fullysyntheticsmall-moleculeinhibitoroftheheatshockproteinHsp90.MolCancerTher.2009Apr;8(4):921-9.PubMedPMID:19372565.
MedKoo 美帝药库公司以药物化学合成技术为核心,密切结合全球抗癌新药研发领域中的新技术、新理论、新趋势和新的发展方向,不断推出抗癌化合物新品种。 。
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美帝药库的药物化合物来源于以下几个渠道:自主合成、委托化学合成、合作伙伴、和从国内外市场上选购。
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(1)上市抗癌药库:该库将含有大约100个全球已批准上市的小分子抗癌化合物;
(2)抗癌候选药物库:该分子库含有大约400个世界各国正在临床研究中抗癌小分子候选药物;
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