Dacomitinib

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Cat.No. 6231 - Dacomitinib | C24H25ClFN5O2 | CAS No. 1110813-31-4
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
Literature

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.

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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Product Datasheets

Safety Datasheet

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


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Keywords: Dacomitinib ErbB inhibitors inhibits EGFR ERBB2 ERBB4 potent irreversible pan-ErbB cancer orally bioavailable PF00299804 EGFR

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