Dacomitinib

Name: Dacomitinib
Brand: Tocris Bioscience
SKU: 6231

Tocris Bioscience, part of Bio-Techne | Catalog # 6231

Citations (3)

COA / SDS

Potent irreversible pan ErbB inhibitor

Key Product Details

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)
Molecular Weight:	469.94

View Full Technical Details for Dacomitinib

Technical Data
Citations

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 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.

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.

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