Chemical Name:N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]
-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine
dihydrochloride
Biological Activity:
Potent inhibitor of epidermal growth factor
receptor (EGFR) tyrosine kinase (IC50 = 3 nM). Displays ~ 100-fold
lower potency against Her2 (IC50 = 290 nM) and is selective over a
range of other related tyrosine kinases (IC50 > 10 μM). Blocks
downstream EGFR signalling events such as MAPKK/MAPK activation. Oral
administration inhibits growth of established human xenografts in athymic
mice.
