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); effective in mouse models of lung cancer driven by EGFRT790M

WZ4002 – 10 mg

Brand:
Cayman
CAS:
1213269-23-8
Storage:
-20
UN-No:
Non-Hazardous - /

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.{27827,27829} 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).{27829,27826} It preferentially targets cells expressing EGFRT790M over those expressing EGFR without the T790M mutation.{27829} WZ4002 is also bioavailable in vivo when given intravenously and is effective in mouse models of lung cancer driven by EGFRT790M.{27829} Efficacy may be enhanced when used in combination therapy with inhibitors of Met kinase activity, Bcl-2, or histone deacetylases.{27825,27822,27824,27823}  

 

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Description

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); effective in mouse models of lung cancer driven by EGFRT790M

Formal name: N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide

Synonyms: 

Molecular weight: 495

CAS: 1213269-23-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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