Potent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50
= 3 nM). Displays ~ 100-fold lower potency against ErbB2 (IC50
= 290 nM) and is selective over a range of other related tyrosine kinases (IC50
> 10 μ
M). Blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Oral administration inhibits growth of established human xenografts in athymic mice.
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Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives.
Solca et al.