Chemical Name: N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidinyl)-pyrimido[5,4-d]pyrimidine-2,8-diamine dihydrochloride
Biological Activity Potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM). Displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). Oral administration inhibits growth of established human xenografts in athymic mice.
Soluble to 50 mM in water and to 50 mM in DMSO
Desiccate at +4°C
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