D-3700 Dacomitinib, Free Base, >99%

DCM-103 DCM-102 DCM-101

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• Dacomitinib, also known as PF-00299804, is a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. It irreversibly blocked erbB1 autophosphorylation in A431 human squamous carcinoma cells with an IC50 of 15.1 nM. It had significant antitumor activity in vivo, including marked tumor regressions in a variety of human tumor xenograft models that express and/or overexpress erbB family members or contain the double mutation (L858R/T790M) in erbB1 (EGFR) associated with resistance to gefitinib and erlotinib. Gonzales A.J., et al. "Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor." Mol. Cancer Ther. 7: 1880-1889 (2008).
• A phase 2 clinical trial demonstrated that dacomitinib had clinical activity in recurrent/metastatic squamous-cell carcinoma of the head and neck (RM-SCCHN). Its toxicity was generally manageable with dose adjustments and interruptions. Abdul Razak A.R., et al. "A phase II trial of dacomitinib, an oral pan-human EGF receptor (HER) inhibitor, as first-line treatment in recurrent and/or metastatic squamous-cell carcinoma of the head and neck." Ann. Oncol. 24: 761-769 (2013).
• A phase 2 clinical trial demonstrated that dacomitinib significantly improved progression-free survival (PFS) versus erlotinib with acceptable toxicity in patients with advanced non-small-cell lung cancer. PFS benefit was shown in most clinical and molecular subsets, notably KRAS wild-type/EGFR any status, KRAS wild-type/EGFR wild-type, and EGFR mutants. Ramalingam S.S., et al. "Randomized phase II study of dacomitinib (PF-00299804), an irreversible pan-human epidermal growth factor receptor inhibitor, versus erlotinib in patients with advanced non-small-cell lung cancer." J. Clin. Oncol. 30: 3337-3344 (2012).
• Related CAS numbers: 1042385-75-0 for the hydrate (1:1).
• Dacomitinib is the active ingredient in the drug product sold under the trade name Vizimpro®.  This drug is currently approved in at least one country for first-line treatment of patients with metastatic non-small cell lung cancer with epidermal growth factor receptor.  NOTE:  THE DACOMITINIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT VIZIMPRO®, AND IS NOT FOR HUMAN USE.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.