Description
Dacomitinib (PF299804,PF-00299804) can inhibit ErbB1, ErbB2, and ErbB4.
Storage
2 years at -20centigrade Powder
Targets
ErbB1, ErbB2, ErbB4
Molecular Formula
C24H25ClFN5O2
Chemical Name
(E)-N-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl)-4-(piperidin-1-yl)but-2-enamide
Solubility
DMSO 19 mg/mL Water
In vitro
As a potent, orally available, irreversible inhibitor of tyrosine kinase, PF299804 can inhibit epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4 with IC50 of 6.0, 45.7 and 73.7nM. Comparing PF299804 to the other three inhibitors (Gefitinib, Erlotinib, and CI-1033), PF299804 shows its characteristics.
In vivo
PF00299804 is effective in gefitinib-sensitive and gefitinib-resistant NSCLC cell lines.Whereas we observed a 70-fold range (4.1-306 nmol/L) in the IC50 for gefitinib against the five most common exon 19 deletions, the IC50 values were between 1 and 2 nmol/L for PF00299804 for all five mutations.
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