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Dacomitinib

Cat. No. 6231 Submit a Review Datasheet / COA / SDS
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Description: Potent irreversible pan ErbB inhibitor
Alternative Names: PF00299804
Chemical Name: (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Dacomitinib

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.

Compound Libraries for Dacomitinib

Dacomitinib is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Dacomitinib

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Dacomitinib

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 46.99 100
DMSO 46.99 100

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 will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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References for Dacomitinib

References are publications that support the biological activity of the product.

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 gefi. 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

If you know of a relevant reference for Dacomitinib, please let us know.

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Citations for Dacomitinib

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.