Cayman WZ4002

The recurrent missense mutation T790M in the kinase domain of epidermal growth factor receptor (EGFR) is a gatekeeper mutation, as it sterically hinders binding of inhibitors while preserving catalytic activity.^1,2 WZ4002 is an irreversible EGFR tyrosine kinase inhibitor that blocks ATP-dependent autophosphorylation of EGFR carrying the T790M mutation as well as an L858R mutation (IC₅₀ = 8 nM).^2,3 It preferentially targets cells expressing EGFR^T790M over those expressing EGFR without the T790M mutation.² WZ4002 is also bioavailable in vivo when given intravenously and is effective in mouse models of lung cancer driven by EGFR^T790M.² Efficacy may be enhanced when used in combination therapy with inhibitors of Met kinase activity, Bcl-2, or histone deacetylases.^4,5,6,7

WARNING This product is not for human or veterinary use.