FR180204isanovelandselectiveinhibitorofextracellularsignal-regulatedkinase(ERK),whichmaybeapotentialnewtherapyforrheumatoidarthritis.FR180204showedactivitytoinhibitERKs(IC50valuesare0.14and0.31μMforERK2andERK1respectively).MedKooCat#:406556Name:FR180204CAS#:865362-74-9ChemicalFormula:C18H13N7ExactMass:327.12324MolecularWeight:327.34ElementalAnalysis:C,66.04;H,4.00;N,29.95Synonym:FR180204;FR-180204;FR180204.IUPAC/ChemicalName:5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amineInChiKey:XVECMUKVOMUNLE-UHFFFAOYSA-NInChiCode:InChI=1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)SMILESCode:NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21TechnicalDataAppearance:SolidpowderPurity:>98%(orrefertotheCertificateofAnalysis)ShippingCondition:Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.StorageCondition:Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).Solubility:SolubleinDMSO,notinwaterShelfLife:>2yearsifstoredproperlyDrugFormulation:ThisdrugmaybeformulatedinDMSOStockSolutionStorage:0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).HarmonizedSystemCode:293490AdditionalInformation     References1:DiricanA,AtmacaH,BozkurtE,ErtenC,KaracaB,UsluR.NovelcombinationofdocetaxelandthymoquinoneinducessynergisticcytotoxicityandapoptosisinDU-145humanprostatecancercellsbymodulatingPI3K-AKTpathway.ClinTranslOncol.2014Jul25.[Epubaheadofprint]PubMedPMID:25060568.2:SreekanthGP,ChuncharuneeA,SirimontapornA,PanaamponJ,SrisawatC,MorchangA,MalakarS,ThuwajitP,KooptiwutS,SuttitheptumrongA,SongprakhonP,NoisakranS,YenchitsomanusPT,LimjindapornT.RoleofERK1/2signalingindenguevirus-inducedliverinjury.VirusRes.2014Aug8;188:15-26.doi:10.1016/j.virusres.2014.03.025.Epub2014Apr1.PubMedPMID:24704674.3:YuenN,LamTI,WallaceBK,KlugNR,AndersonSE,O'DonnellME.Ischemicfactor-inducedincreasesincerebralmicrovascularendothelialcellNa/Hexchangeactivityandabundance:evidenceforinvolvementofERK1/2MAPkinase.AmJPhysiolCellPhysiol.2014May15;306(10):C931-42.doi:10.1152/ajpcell.00021.2013.Epub2014Mar19.PubMedPMID:24647544;PubMedCentralPMCID:PMC4024711.4:BilslandAE,StevensonK,LiuY,HoareS,CairneyCJ,RoffeyJ,KeithWN.Mathematicalmodelofatelomerasetranscriptionalregulatorynetworkdevelopedbycell-basedscreening:analysisofinhibitoreffectsandtelomeraseexpressionmechanisms.PLoSComputBiol.2014Feb13;10(2):e1003448.doi:10.1371/journal.pcbi.1003448.eCollection2014Feb.PubMedPMID:24550717;PubMedCentralPMCID:PMC3923661.5:ChoiNY,ChoiH,ParkHH,LeeEH,YuHJ,LeeKY,JooLeeY,KohSH.Neuroprotectiveeffectsofamlodipinebesylateandbenidipinehydrochlorideonoxidativestress-injuredneuralstemcells.BrainRes.2014Mar10;1551:1-12.doi:10.1016/j.brainres.2014.01.016.Epub2014Jan16.PubMedPMID:24440775.6:ThalerCD,MiyataH,HaimoLT,CardulloRA.WaveformgenerationiscontrolledbyphosphorylationandswimmingdirectioniscontrolledbyCa2+inspermfromthemosquitoCulexquinquefasciatus.BiolReprod.2013Dec12;89(6):135.doi:10.1095/biolreprod.113.109488.Print2013Dec.PubMedPMID:24108305.7:AnastassiADIsT,Duong-LyKC,DeaconSW,LafontantA,MaH,DevarajanK,DunbrackRLJr,WuJ,PetersonJR.Ahighlyselectivedualinsulinreceptor(IR)/insulin-likegrowthfactor1receptor(IGF-1R)inhibitorderivedfromanextracellularsignal-regulatedkinase(ERK)inhibitor.JBiolChem.2013Sep27;288(39):28068-77.doi:10.1074/jbc.M113.505032.Epub2013Aug9.PubMedPMID:23935097;PubMedCentralPMCID:PMC3784719.8:SunagaN,KairaK,ImaiH,ShimizuK,NakanoT,ShamesDS,GirardL,SohJ,SatoM,IwasakiY,IshizukaT,GazdarAF,MinnaJD,MoriM.OncogenicKRAS-inducedepiregulinoverexpressioncontributestoaggressivephenotypeandisapromisingtherapeutictargetinnon-small-celllungcancer.Oncogene.2013Aug22;32(34):4034-42.doi:10.1038/onc.2012.402.Epub2012Sep10.PubMedPMID:22964644.9:DoghmanM,LalliE.EfficacyofthenoveldualPI3-kinase/mTORinhibitorNVP-BEZ235inapreclinicalmodelofadrenocorticalcarcinoma.MolCellEndocrinol.2012Nov25;364(1-2):101-4.doi:10.1016/j.mce.2012.08.014.Epub2012Aug31.PubMedPMID:22960230.10:RagusaM,StatelloL,MaugeriM,MajoranaA,BarbagalloD,SalitoL,SammitoM,SantonocitoM,AngelicaR,CavallaroA,ScaliaM,CaltABIanoR,PriviteraG,BiondiA,DiVitaM,CappellaniA,VasquezE,LanzafameS,TendiE,CelesteS,DiPietroC,BasileF,PurrelloM.SpecificalterationsofthemicroRNAtranscriptomeandglobalnetworkstructureincolorectalcanceraftertreatmentwithMAPK/ERKinhibitors.JMolMed(Berl).2012Dec;90(12):1421-38.doi:10.1007/s00109-012-0918-8.Epub2012Jun4.PubMedPMID:22660396.