Dacomitinib

Key Product Details

Product Description

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Product Specifications for Dacomitinib

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Dacomitinib

The following data is based on the product molecular weight 469.94.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.13 mL	10.64 mL	21.28 mL
5 mM	0.43 mL	2.13 mL	4.26 mL
10 mM	0.21 mL	1.06 mL	2.13 mL
50 mM	0.04 mL	0.21 mL	0.43 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 3 publications citing the usage of this product.

• Gonzales Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol.Cancer.Ther. 2008 PMID: 18606718
• Li A ROR1-HER3-lncRNA signalling axis modulates the Hippo-YAP pathway to regulate bone metastasis. Nat.Cell.Biol. 2017 PMID: 28114269
• Engelman PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefi. Cancer.Res. 2007 PMID: 18089823

Product Documents for Dacomitinib