LKT Labs

Biochemicals for Life Science Research

Dacomitinib Monohydrate

Product ID D0006
Cas No. 1042385-75-0
Purity ≥99%
Product Unit SizeCostQuantityStock
1 mg $93.70 In stock
5 mg $181.30 In stock
25 mg $481.40 In stock
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Description

Dacomitinib is an ATP-competitive, irreversible pan-erbB receptor (EGFR) inhibitor that shows anticancer chemotherapeutic activity in models of squamous cell carcinoma, ovarian carcinoma, and non-small-cell lung cancer (NSCLC). Dacomitinib covalently modifies cytosine residues in the catalytic domain of this kinase, preventing phosphorylation of downstream targets such as Akt, and ERK, resulting in cell cycle arrest at the G0/G1 phase and induction of apoptosis. This compound also inhibits mutant EGF receptors in drug-resistant in vivo tumor models.

Product Info

Cas No.

1042385-75-0
Purity

≥99%
Formula

C24H25ClFN5O2 • H2O
Formula Wt.

487.95
Chemical Name

(E)-N-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]-4- piperidin-1-ylbut-2-enamide;hydrate
IUPAC Name

(E)-N-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]-4- piperidin-1-ylbut-2-enamide;hydrate
Synonym

PF-00299804
Solubility

Soluble in water (<1 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), DMSO (19 mg/ml at 25 °C), and 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 9 (10 mg/ml at 25 °C).
Appearance

off-white powder

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

MSDS

D0006 MSDS PDF
Info Sheet

D0006 Info Sheet PDF

References

Kalous O, Conklin D, Desai AJ, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib. Mol Cancer Ther. 2012 Sep;11(9):1978-87. PMID: 22761403.

Gonzales AJ, Hook KE, Althaus IW, et al. Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2008 Jul;7(7):1880-9. PMID: 18606718.

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