PF299804 (Dacomitinib, PF299)

Catalog No.: A11051

EGFR inhibitor

PF299804 (Dacomitinib, PF299)

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
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Warning Products are for laboratory research use only. Not for human use. We do not sell to patients.
  • 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 nM45.7 nM73.7 nM
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.
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.

Catalog Num A11051
Actions Inhibitor
CAS No. 1110813-31-4
Formula C24H25ClFN5O2
M. Wt 469.9
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.

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