MedKoo Biosciences/Pazopanib/202161/100mg

Synonym:GW786034;GW786034;GW786034;Pazopanib;USbrandname:Votrient.

IUPAC/ChemicalName:5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide

InChiKey:CUIHSIWYWATEQL-UHFFFAOYSA-N

InChiCode:InChI=1S/C21H23N7O2S/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25)

SMILESCode:O=S(C1=CC(NC2=NC=CC(N(C3=CC4=NN(C)C(C)=C4C=C3)C)=N2)=CC=C1C)(N)=O

TechnicalData

AdditionalInformation

Pazopanibhydrochlorideisawhitetoslightlyyellowsolid.ItisveryslightlysolubleatpH1andpracticallyinsolubleabovepH4inaqueousmedia.TabletsofVOTRIENTarefororaladmiNISTration.Each200mgtabletofVOTRIENTcontains216.7mgofpazopanibhydrochloride,equivalentto200mgofpazopanibfreebase.TheinactiveingredientsofVOTRIENTare:TabletCore:Magnesiumstearate,microcrystallinecellulose,povidone,sodiumstarchglycolate.Coating:Grayfilm-coat:Hypromellose,ironoxideblack,macrogol/polyethyleneglycol400(PEG400),polysorbate80,titaniumdioxide.
 
Pazopanibisamulti-tyrosinekinaseinhibitorofvascularendothelialgrowthfactorreceptor(VEGFR)-1,VEGFR-2,VEGFR-3,platelet-derivedgrowthfactorreceptor(PDGFR)-αand-β,fibroblastgrowthfactorreceptor(FGFR)-1and-3,cytokinereceptor(Kit),interleukin-2receptorinducIBLeT-cellkinase(Itk),leukocyte-specificproteintyrosinekinase(Lck),andtransmembraneglycoproteinreceptortyrosinekinase(c-Fms).Invitro,pazopanibinhibitedligand-inducedautophosphorylationofVEGFR-2,KitandPDGFR-βreceptors.Invivo,pazopanibinhibitedVEGF-inducedVEGFR-2phosphorylationinmouselungs,angiogenesisinamousemodel,andthegrowthofsomehumantumorxenograftsinmice
 
 

References

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3:SiderasK,MenefeeME,BurtonJK,ErlichmanC,BibleKC,IvySP.ProfoundHairandSkinHypopigmentationinanAfricanAmericanWomanTreatedWiththeMulti-TargetedTyrosineKinaseInhibitorPazopanib.JClinOncol.2010Jun1.[Epubaheadofprint]PubMedPMID:20516434.

4:TailorTD,HannaG,YarmolenkoPS,DreherMR,BetofAS,NixonAB,SpasojevicI,DewhirstMW.Effectofpazopanibontumormicroenvironmentandliposomedelivery.MolCancerTher.2010Jun;9(6):1798-808.Epub2010Jun1.PubMedPMID:20515941.

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6:BöhmS,HessD,GillessenS,BrändleM.Improvedglycemiccontrolwiththemulti-receptortyrosinekinaseinhibitorpazopanib.DiabetesCare.2010Jun;33(6):e82.PubMedPMID:20508227.

7:SternbergCN.Pazopanibinrenalcellcarcinoma.ClinAdvHematolOncol.2010Apr;8(4):232-3.PubMedPMID:20505644.