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Description
Dacomitinib is an ATP-competitive, irreversible pan-erbB receptor tyrosine kinase (EGFR) inhibitor that shows anticancer activity in models of squamous cell carcinoma, ovarian carcinoma, and non-small-cell lung cancer. Dacomitinib covalently modifies cytosine residues in the catalytic domain of this kinase, preventing phosphorylation of downstream targets such as HER, AKT, and ERK, resulting in cell cycle arrest at the G0/G1 phase and induction of apoptosis. This compound also inhibits mutant EGF receptors in drug-resistant in vivo tumor models.
Specifications
Cas No. 1042385-75-0
Product ID D0006
Product Name Dacomitinib
Synonym PF-00299804
Formula Wt. 487.95
Purity >99%
Solubility In DMSO
Store Temp -20°C
References
Kalous O, Conklin D, Desai AJ, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib. Mol Cancer Ther. 2012 Sep;11(9):1978-87. PMID: 22761403.
Gonzales AJ, Hook KE, Althaus IW, et al. Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2008 Jul;7(7):1880-9. PMID: 18606718. |