Dacomitinib
Chemical Name: (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide
Purity: ≥98%
Biological Activity
Dacomitinib is a potent irreversible pan ErbB inhibitor (IC50 values are 6.0, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively). Inhibits mutant and wild type forms of ErbB, including EGFR T780M, and shows activity in NSCLC cell lines sensitive and resistant to Iressa (Cat. No. 3000). Inhibits tumor growth. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
-
Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor.
Gonzales et al.
Mol.Cancer.Ther., 2008;7:1880 -
A ROR1-HER3-lncRNA signalling axis modulates the Hippo-YAP pathway to regulate bone metastasis.
Li et al.
Nat.Cell.Biol., 2017;19:106 -
PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefi.
Engelman et al.
Cancer.Res., 2007;67:11924
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