Biological Activity
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.
Technical Data
| M. Wt | 469.94 |
| Formula | C24H25ClFN5O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1110813-31-4 |
| PubChem ID | 11511120 |
| InChI Key | LVXJQMNHJWSHET-AATRIKPKSA-N |
| Smiles | O=C(/C=C/CN1CCCCC1)NC2=C(OC)C=C(N=CN=C3NC4=CC=C(F)C(Cl)=C4)C3=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 46.99 | 100 | |
| DMSO | 46.99 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 469.94. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
Engelman et al (2007) PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer.Res. 67 11924 PMID: 18089823
Gonzales et al (2008) Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol.Cancer.Ther. 7 1880 PMID: 18606718
Li et al (2017) A ROR1-HER3-lncRNA signalling axis modulates the Hippo-YAP pathway to regulate bone metastasis. Nat.Cell.Biol. 19 106 PMID: 28114269
Keywords: Dacomitinib, supplier, Dacomitinib, ErbB, inhibitors, inhibits, EGFR, ERBB2, ERBB4, potent, irreversible, pan-ErbB, cancer, orally, bioavailable, PF00299804, EGFR, Tocris Bioscience
