RelatedCAS#: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-N

InChiCode: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*1H

SMILESCode:ClC1=CC=C(NC2=NN=C(CC3=CC=NC=C3)C4=C2C=CC=C4)C=C1.[H]Cl.[H]Cl

TechnicalData

AdditionalInformation

RelatedCAS#
212141-51-0(Vatalanib2HCl);
212141-54-3(Vatalanib);
212142-18-2(Vatalanibsuccinate).

References

1: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.Epub2011Apr4.PubMedPMID:21464409.

11:Kłosowska-WardęgaA,HasumiY,AhgrenA,HeldinCH,HellbergC.Combinationtherapyusingimatinibandvatalanibimprovesthetherapeuticefficiencyofpaclitaxeltowardsamousemelanomatumor.MelanomaRes.2010Oct21.[Epubaheadofprint]PubMedPMID:20975605.

12:GerstnerER,EichlerAF,PlotkinSR,DrappatzJ,DoyleCL,XuL,DudaDG,WenPY,JainRK,BatchelorTT.PhaseItrialwithbioMarkerstudiesofvatalanib(PTK787)inpatientswithnewlydiagnosedglioblastomatreatedwithenzymeinducinganti-epilepticdrugsandstandardrADIationandtemozolomide.JNeurooncol.2011Jun;103(2):325-32.doi:10.1007/s11060-010-0390-7.Epub2010Sep7.PubMedPMID:20821342.

13:ZhangYH,YueZJ,ZhangH,TangGS,WangY,LiuJM.Temozolomide/PLGAmicroparticlesplusvatalanibinhibitstumorgrowthandangiogenesisinanorthotopicgliomamodel.EurJPharmBiopharm.2010Nov;76(3):371-5.doi:10.1016/j.ejpb.2010.08.011.Epub2010Sep9.PubMedPMID:20816959.

14:CookN,BasuB,BiswasS,KareclasP,MannC,PalmerC,ThomasA,NicholsonS,MorganB,LomasD,SirohiB,ManderAP,MiddletonM,CorriePG.Aphase2studyofvatalanibinmetastaticmelanomapatients.EurJCancer.2010Oct;46(15):2671-3.doi:10.1016/j.ejca.2010.07.014.Epub2010Aug25.PubMedPMID:20800475.

15:PaeslerJ,GehrkeI,GandhirajanRK,FilipovichA,HertweckM,ErdfelderF,UhrmacherS,Poll-WolbeckSJ,HallekM,KreuzerKA.Thevascularendothelialgrowthfactorreceptortyrosinekinaseinhibitorsvatalanibandpazopanibpotentlyinduceapoptosisinchroniclymphocyticleukemiacellsinvitroandinvivo.ClinCancerRes.2010Jul1;16(13):3390-8.doi:10.1158/1078-0432.CCR-10-0232.Epub2010Jun22.PubMedPMID:20570929.

16:Jaeger-LanskyA,CejkaD,YingL,PreusserM,HoeflmayerD,FuerederT,KoehrerS,WacheckV.EffectsofvatalanibontumorgrowthcanbepotentiatedbymTORblockadeinvivo.CancerBiolTher.2010Jun;9(11):919-27.Epub2010Jun18.PubMedPMID:20404549.

17:ChioreanEG,MalireddyS,YoungerAE,JonesDR,WaddellMJ,SloopMI,YuM,HallSD,SchneiderB,SweeneyCJ.AphaseIdoseescalationandpharmacokineticstudyofvatalanib(PTK787/ZK222584)incombinationwithpaclitaxelinpatientswithadvancedsolidtumors.CancerChemotherPharmacol.2010Aug;66(3):441-8.doi:10.1007/s00280-009-1179-2.Epub2009Nov29.PubMedPMID:20091169.

18:LankheetAG,HillebrandMJ,LangenbergMH,RosingH,HuitemaAD,VoestEE,SchellensJH,BeijnenJH.AvalidatedassayforthequantitativeanalysisofvatalanibinhumanEDTAplasmabyliquidchromatographycoupledwithelectrosprayionizationtandemmassspectrometry.JChromatogrBAnalytTechnolBiomedLifeSci.2009Nov1;877(29):3625-30.doi:10.1016/j.jchromb.2009.09.001.Epub2009Sep6.PubMedPMID:19762293.

19:ReardonDA,EgorinMJ,DesjardinsA,VredenburghJJ,BeumerJH,LagattutaTF,GururanganS,HerndonJE2nd,SalvadoAJ,FriedmanHS.PhaseIpharmacokineticstudyofthevascularendothelialgrowthfactorreceptortyrosinekinaseinhibitorvatalanib(PTK787)plusimatinibandhydroxyureaformalignantglioma.Cancer.2009May15;115(10):2188-98.doi:10.1002/cncr.24213.PubMedPMID:19248046;PubMedCentralPMCID:PMC2691174.

20:LosM,RoodhartJM,VoestEE.Targetpractice:lessonsfromphaseIIItrialswithbevacizumabandvatalanibinthetreatmentofadvancedcolorectalcancer.Oncologist.2007Apr;12(4):443-50.Review.PubMedPMID:17470687.