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Potentinhibitorofepidermalgrowthfactorreceptor(EGFR)tyrosinekinase(IC50=3nM).Displays~100-foldlowerpotencyagainstErbB2(IC50=290nM)andisselectiveoverarangeofotherrelatedtyrosinekinases(IC50>10μM).BlocksdownstreamEGFRsignalingeventssuchasMAPKK/MAPKactivation.OraladmiNISTrationinhibitsgrowthofestablishedhumanxenograftsinathymicmice.
BIBU1361dihydrochlorideisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight516.87.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Solcaetal(2004)Inhibitionofepidermalgrowthfactorreceptoractivitybytwopyrimidopyrimidinederivatives.J.Pharmacol.Exp.Ther.311502PMID:15199094
Keywords:BIBU1361dihydrochloride,supplier,Selective,inhibitors,inhibits,EGFR-kinases,Epidermal,Growth,Factors,Receptors,ErbB,Her,Receptor,Tyrosine,Kinases,RTKs,BIBU1361,dihydrochloride,EGFR,EGFR,TocrisBioscience
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