Description
AS-703026isaninhibitorofMEK1/2thatexhibitsanticancerchemotherapeuticactivity.Invitro,AS-703026inhibitsproliferationofmelanomacells.InbothinvitroandinvivomodelsofcolorectalcancercontainingWTRasormutantKRAS,AS-703026inhibitsgrowthofcellsandalsooftumors.Additionally,AS-703026inhibitsgrowthandsurvivalofmultiplemyelomacellsbyinducingactivationofcaspase3,cleavageofpoly(ADP)-ribosepolymerase(PARP),andapoptosis;thiscompoundsuppressestumorgrowthanddecreasesmicrovesselnumbersinanimalmodelsaswell.
References
ParkSJ,HongSW,MoonJH,etal.TheMEK1/2inhibitorAS703026circumventsresistancetotheBRAFinhibitorPLX4032inhumanmalignantmelanomacells.AmJMedSci.2013Dec;346(6):494-8.PMID:24051957.
YoonJ,KooKH,ChoiKY.MEK1/2inhibitorsAS703026andAZD6244maybepotentialtherapiesforKRASmutatedcolorectalcancerthatisresistanttoEGFRmonoclonalantibodytherapy.CancerRes.2011Jan15;71(2):445-53.PMID:21118963.
KimK,KongSY,FulcinitiM,etal.BlockadeoftheMEK/ERKsignallingcascadebyAS703026,anovelselectiveMEK1/2inhibitor,inducespleiotropicanti-myelomaactivityinvitroandinvivo.BrJHaematol.2010May;149(4):537-49.PMID:20331454.
