BIBU 1361 dihydrochloride
Chemical Name: N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride
Biological ActivityPotent 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 μM). Blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Oral administration inhibits growth of established human xenografts in athymic mice.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives.
Solca et al.
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