• SpecificandpotentJAK-2proteintyrosinekinaseinhibitor.AlsoinhibitsEGFreceptorautophosphorylation,withanIC50of100nM.InhibitsDNAsynthesisandcellgrowth;inducesapoptosis.Levitzki,A."Tyrphostins--potentialantiproliferativeagentsandnovelmoleculartools."Biochem.Pharmacol.40:913-918(1990).Gazit,A.,etal."Tyrphostins.2.Heterocyclicandalpha-substitutedbenzylidenemalononitriletyrphostinsaspotentinhibitorsofEGFreceptorandErbB2/neutyrosinekinases."J.Med.Chem.34:1896-1907(1991).
• Inhibitsthegrowthofleukemiccellsinvitroandinvivo.BlocksSTAT3constitutiveactivationandinhibitsbothinterleukin2(IL2)-inducedandspontaneousgrowthofMycosisfungoides(MF),acutaneousTcelllymphoma.GrowthofhumanovarianandbreastcancercelllineswasshowntobesignificantlysuppressedbyAG490viaJAK/STAT3pathwayinhibition.Meydan,N.,etal."InhibitionofacutelymphoblasticleukaemiabyaJak-2inhibitor."Nature379:645-648(1996).NielsenM.,etal."ConstitutiveactivationofaslowlymigratingisoformofStat3inmycosisfungoides:tyrphostinAG490inhibitsStat3activationandgrowthofmycosisfungoidestumorcelllines."ProcNatlAcadSciUSA.94:6764-6769(1997).Eriksen,K.W.,etal."ConstitutiveSTAT3-activationinSezarysyndrome:tyrphostinAG490inhibitsSTAT3-activation,interleukin-2receptorexpressionandgrowthofleukemicSezarycells."Leukemia15:787-793(2001).BurkeW.M.,etal."InhibitionofconstitutivelyactiveStat3suppressesgrowthofhumanovarianandbreastcancercells."Oncogene20:7925-7934(2001).Levitzki,A."Tyrosinekinasesastargetsforcancertherapy."EurJCancer38Suppl5:S11-S18(2002).BurdelyaL.,etal."CombinationtherapywithAG-490andinterleukin12achievesgreaterantitumoreffectsthaneitheragentalone."MolCancerTher11:893-899(2002).
• AG490isaJAK3/STAT,JAK3/AP-1,andJAK3/MAPKsignalingpathwayinhibitorandalsoblocksJAK3autophosphorylation.Kirken,R.A.,etal."TyrphostinAG-490inhibitscytokine-mediatedJAK3/STAT5a/bsignaltransductionandcellularproliferationofantigen-activatedhumanTcells."J.Leukoc.Biol.65:891-899(1999).Wang,L.H.,etal."JAK3,STAT,andMAPKsignalingpathwaysasnovelmoleculartargetsforthetyrphostinAG-490regulationofIL-2-mediatedTcellresponse."J.Immunol.162:3897-3904(1999).DeVos,J.,etal."JAK2tyrosinekinaseinhibitortyrphostinAG490downregulatesthemitogen-activatedproteinkinase(MAPK)andsignaltransducerandactivatoroftranscription(STAT)pathwaysandinducesapoptosisinmyelomacells."Br.J.Haematol.109:823-828(2000).
• Previouslysoldas"TyrphostinB42";thecatalognumberhasnotchanged.
• PleaserequestTechnicalNote#22foradditionalinformation.
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,medical,veterinary,food,orhouseholduse.

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