PF-00299804 Dacomitinib

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Chemical Information

Product name：PF-00299804 Dacomitinib	Purity：98% min
CAS NO：1042385-75-0	Solubility：DMSO : 50 mg/mL (106.40 mM)
Molecular Formula：C₂₄H₂₇ClFN₅O₃	Package：Package according to customer requirements
Molecular Weight：487.954	Storage：Store at -20℃

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Remarks

Dacomitinib, aslo known as PF-299 and PF-00299804 ; or PF299804, is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. Dacomitinib specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells. EGFRs play major roles in tumor cell proliferation and tumor vascularization, and are often overexpressed or mutated in various tumor cell types.

References

[1]. Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res. 2007 Dec 15;67(24):11924-32.

[2]. Kalous O, 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.