Vatalanib,alsoknownasPTK787,isanorallybioavailableanilinophthalazinewithpotentialantineoplasticactivity.Vatalanibbindstoandinhibitstheproteinkinasedomainofvascularendothelialgrowthfactorreceptors1and2;bothreceptortyrosinekinasesareinvolvedinangiogenesis.Thisagentalsobindstoandinhibitsrelatedreceptortyrosinekinases,includingplatelet-derivedgrowthfactor(PDGF)receptor,c-Kit,andc-Fms.MedKooCat#:203110Name:VatalanibHClCAS#:212141-51-0ChemicalFormula:C20H17Cl3N4ExactMass:346.09852MolecularWeight:419.73ElementalAnalysis:C,57.23;H,4.08;Cl,25.34;N,13.35RelatedCAS#:212141-51-0(HCl) 212141-54-3(freebase) 212142-18-2(succinate) Synonym:PTK787;PTK787;PTK-787;ZK222584;ZK222584;ZK-222584;CGP79787;CGP-797870;ZK-232934;CGP79787D;PTK787/ZK222584;CGP-7978.IUPAC/ChemicalName:N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-aminedihydrochloride.InChiKey:AZUQEHCMDUSRLH-UHFFFAOYSA-NInChiCode:InChI=1S/C20H15ClN4.2ClH/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14;;/h1-12H,13H2,(H,23,25);2*1HSMILESCode:ClC1=CC=C(NC2=NN=C(CC3=CC=NC=C3)C4=C2C=CC=C4)C=C1.[H]Cl.[H]ClTechnicalDataAppearance:Whitetooff-whitecrystallinesolidPurity:>98%(orrefertotheCertificateofAnalysis)CertificateofAnalysis:ViewCoA:currentbatch,Lot#LC50701SafetyDataSheet(MSDS):ViewMaterialSafetyDataSheet(MSDS)ShippingCondition:Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.StorageCondition:Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).Solubility:solubleinDMSO,notsolubleinwater.ShelfLife:>10yearsifstoredproperlyDrugFormulation:ThisdrugmaybeformulatedinDMSOStockSolutionStorage:0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).HarmonizedSystemCode:293490AdditionalInformationRelatedCAS#212141-51-0(Vatalanib2HCl);212141-54-3(Vatalanib);212142-18-2(Vatalanibsuccinate).References1:GiatromanolakiA,KoukourakisMI,SivridisE,GatterKC,TrarbachT,FolprechtG,ShiMM,LebwohlD,JalavaT,LaurentD,MeinhardtG,HarrisAL;TumourandAngiogenesisResearchGroup.Vasculardensityanalysisincolorectalcancerpatientstreatedwithvatalanib(PTK787/ZK222584)intherandomisedCONFIRMtrials.BrJCancer.2012Sep25;107(7):1044-50.doi:10.1038/bjc.2012.369.Epub2012Aug21.PubMedPMID:22910317;PubMedCentralPMCID:PMC3461163.2:WilsonPM,YangD,AzumaM,ShiMM,DanenbergKD,LebwohlD,SherrodA,LadnerRD,ZhangW,DanenbergPV,TrarbachT,FolprechtG,MeinhardtG,LenzHJ.IntratumoralexpressionprofilingofgenesinvolvedinangiogenesisincolorectalcancerpatientstreatedwithchemotherapyplustheVEGFRinhibitorPTK787/ZK222584(vatalanib).PharmacogenomicsJ.2012Jun5.doi:10.1038/tpj.2012.23.[Epubaheadofprint]PubMedPMID:22664478.3:LiuS,XuC,LiG,LiuH,XieJ,TuG,PengH,QiuS,LiangS.VatalanibdecreasethepositiveinteractionofVEGFreceptor-2andP2X(2/3)receptorinchronicconstrictioninjuryrats.NeuRochemInt.2012May;60(6):565-72.doi:10.1016/j.neuint.2012.02.006.Epub2012Feb15.PubMedPMID:22361062.4:JonesSF,SpigelDR,YardleyDA,ThompsonDF,BurrisHA3rd.AphaseItrialofvatalanib(PTK/ZK)incombinationwithbevacizumabinpatientswithrefractoryand/oradvancedmalignancies.ClinAdvHematolOncol.2011Nov;9(11):845-52.PubMedPMID:22252616.5:JahanT,GuL,KratzkeR,DudekA,OttersonGA,WangX,GreenM,VokesEE,KindlerHL.Vatalanibinmalignantmesothelioma:aphaseIItrialbytheCancerandLeukemiaGroupB(CALGB30107).LungCancer.2012Jun;76(3):393-6.doi:10.1016/j.lungcan.2011.11.014.Epub2011Dec22.PubMedPMID:22197613.6:KoukourakisMI,GiatromanolakiA,SivridisE,GatterKC,TrarbachT,FolprechtG,ShiMM,LebwohlD,JalavaT,LaurentD,MeinhardtG,HarrisAL.Prognosticandpredictiveroleoflactatedehydrogenase5expressionincolorectalcancerpatientstreatedwithPTK787/ZK222584(vatalanib)antiangiogenictherapy.ClinCancerRes.2011Jul15;17(14):4892-900.doi:10.1158/1078-0432.CCR-10-2918.Epub2011Jun1.PubMedPMID:21632858;PubMedCentralPMCID:PMC3145151.7:GaulerTC,BesseB,MauguenA,MericJB,GounantV,FischerB,OverbeckTR,KrisselH,LaurentD,TiainenM,CommoF,SoriaJC,EberhardtWE.PhaseIItrialofPTK787/ZK222584(vatalanib)admiNISTeredorallyonce-dailyorintwodivideddailydosesassecond-linemonotherapyinrelapsedorprogressingpatientswithstageIIIB/IVnon-small-celllungcancer(NSCLC).AnnOncol.2012Mar;23(3):678-87.doi:10.1093/annonc/mdr255.Epub2011May26.PubMedPMID:21617019.8:JoensuuH,DeBraudF,GrignagniG,DePasT,SpitalieriG,CocoP,SpreaficoC,BoselliS,ToffalorioF,BonoP,JalavaT,KappelerC,AgliettaM,LaurentD,CasaliPG.Vatalanibformetastaticgastrointestinalstromaltumour(GIST)resistanttoimatinib:finalresultsofaphaseIIstudy.BrJCancer.2011May24;104(11):1686-90.doi:10.1038/bjc.2011.151.Epub2011May3.PubMedPMID:21540861;PubMedCentralPMCID:PMC3111164.9:SpigelD,JonesS,HainsworthJ,InfanteJ,GrecoFA,ThompsonD,DossH,BurrisH.AphaseItrialtodeterminethesafetyofimatinibincombinationwithvatalanibinpatientswithadvancedmalignancies.CancerInvest.2011May;29(4):308-12.doi:10.3109/07357907.2011.568567.PubMedPMID:21469980.10:SobreroAF,BruzziP.Vatalanibinadvancedcolorectalcancer:twostudieswithidenticalresults.JClinOncol.2011May20;29(15):1938-40.doi:10.1200/JCO.2010.33.2429.Epub201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