Description
CEP-32496isakinaseinhibitorthathasmultikinasebindingactivitybutremainsselectivelycytotoxicformutant(V600E)B-Raf(versusWT);itexhibitsanticancerchemotherapeuticactivity.AlsocontributingtotheABIlityofCEP-32496toinhibitcellproliferation,thiscompoundinhibitspMEKandmERKinanimalmodelswithtumorscontainingthemutantB-Raf.
References
JamesJ,RuggeriB,ArmstrongRC,etal.CEP-32496:anovelorallyactiveBRAF(V600E)inhibitorwithselectivecellularandinvivoantitumoractivity.MolCancerTher.2012Apr;11(4):930-41.PMID:22319199.
RowbottomMW,FaraoniR,ChaoQ,etal.Identificationof1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)ureahydrochloride(CEP-32496),ahighlypotentandorallyefficaciousinhibitorofV-RAFmurinesarcomaviraloncogenehomologueB1(BRAF)V600E.JMedChem.2012Feb9;55(3):1082-105.PMID:22168626.