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PotentdualEGFR/ErbB2tyrosinekinaseinhibitor(IC50valuesare0.01and0.014μMrespectively).SelectivelyinhibitsgrowthofhumantumorcellsoverexpressingEGFRandErbB2(IC50valuesare0.11μMforinhibitionofHN5,N87andBT474tumorcelllinesvs.>30μMforinhibitionofnon-tumorcelllineHFF).Inhibitstumorgrowthinvivoby~80%inamurinexenograftmodelfollowingoraladmiNISTration.
SoldforresearchpurposesunderagreementfromGlaxoSmithKline.
GW583340dihydrochlorideisalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight671.03.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Gauletal(2003)DiscoveryandbiologicalevaluationofpotentdualErbB-2/EGFRtyrosinekinaseinhibitors:6-thiazolylquinazolines.Bioorg.Med.Chem.Lett.13637PMID:12639547
Keywords:GW583340dihydrochloride,supplier,Potent,dual,EGFR,ErbB2,inhibitors,inhibits,orally,active,Epidermal,Growth,Factors,Receptors,Her,Receptor,Tyrosine,Kinases,RTKs,GW583340,dihydrochloride,GlaxoSmithKline,GSK,EGFR,EGFR,TocrisBioscience
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