PF299804 (Dacomitinib, PF299)

Name: PF299804 (Dacomitinib, PF299)
Brand: Adooq Bioscience
SKU: A11051
Rating: 100 (4 reviews)

Catalog No.: A11051

EGFR inhibitor

Product Citations (4)

PF299804 (Dacomitinib, PF299) Chemical Structure

CAS NO. 1110813-31-4

PF299804 is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4.

Availability: In stock

Package	Price	Qty
5 mg	$75.00
10 mg	$130.00
50 mg	$260.00
100 mg	$380.00
10mM * 1mL in DMSO	$110.00
Custom Size	Get quote

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Products are for laboratory research use only. Not for human use. We do not sell to patients.

Adooq Products cited in reputable papers

Publications Citing Use of Adooq PF299804 (Dacomitinib, PF299)

Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358

Biological Activity

PF299804 is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4.

Targets

EGFR (Cell-free assay)	ErbB2 (Cell-free assay)	ErbB4 (Cell-free assay)
6.0 nM	45.7 nM	73.7 nM

Solubility *

In vitro (25°C)	DMSO	17 mg/mL (36.17 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	1% DMSO+30% polyethylene glycol+1% Tween 80, pH 9	9 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	21.28 mL	106.41 mL	212.81 mL
0.5 mM	4.26 mL	21.28 mL	42.56 mL
1 mM	2.13 mL	10.64 mL	21.28 mL
5 mM	0.43 mL	2.13 mL	4.26 mL

*The above data is based on the productmolecular weight 469.9 . 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.

Chemical Properties

Catalog Num	A11051
Actions	Inhibitor
CAS No.	1110813-31-4
Formula	C24H25ClFN5O2
M. Wt	469.9
Solubility	DMSO
Purity	>98%
Synonyms	PF-299804, Dacomitinib, PF-299
SMILES	COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4
Storage	Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.