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Dacomitinib

Catalog No. T2483   CAS 1110813-31-4
Synonyms: PF-299804, PF-00299804, PF299

Dacomitinib (PF299)(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

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Dacomitinib Chemical Structure
Dacomitinib, CAS 1110813-31-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
2 mg In stock $ 45.00
5 mg In stock $ 72.00
10 mg In stock $ 129.00
25 mg In stock $ 183.00
50 mg In stock $ 239.00
100 mg In stock $ 372.00
200 mg In stock $ 468.00
500 mg In stock $ 769.00
1 mL * 10 mM (in DMSO) In stock $ 72.00
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Purity: 100%
Purity: 99.34%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Dacomitinib (PF299)(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
Targets&IC50 EGFR:6.0 nM, ErbB4:73.7 nM, ErbB2:45.7 nM
Kinase Assay ELISA-Based ERBB Kinase Assay: The ERBB1, ERBB 2, and ERBB4 cytoplasmic fusion proteins are made by cloning the ERBB1 sequence (Met-668 to Ala-1211), ERBB2 (Ile-675 to Val-1256), and ERBB4 sequence (Gly-259 to Gly-690) into the baculoviral vector pFastBac using PCR. Proteins are expressed in baculovirusinfected Sf9 insect cells as GST fusion proteins. The proteins are purified by affinity chromatography using glutathione sepharose beads. Inhibition of ERBB tyrosine kinase activity is assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, 125 mM NaCl, 10 mM MgCl2, 100 μM sodium orthovanadate, 2 mM dithiothreitol, 20 μM ATP, PF299804 or vehicle control, and 1-5 nM GST-erbB per 50 μL of reaction mixture) are run in 96-well plates coated with 0.25 mg/mL poly-Glu-Tyr. The reactions are incubated for 6 minutes at room temperature while being shaken. Kinase reactions are stopped by removal of the reaction mixture, and then the wells are washed with wash buffer (0.1% Tween 20 in PBS). Phosphorylated tyrosine residues are detected by adding 0.2 μg/mL antiphosphotyrosine antibody (Oncogene Ab-4; 50 μL/well) coupled to horseradish peroxidase (HRP) diluted in PBS containing 3% BSA and 0.05% Tween 20 for 25 minutes while being shaken at room temperature. The antibody is removed, and plates are washed in wash buffer. HRP substrate (SureBlue3,3?,5,5?-tetramethyl benzidine or TMB) is added (50 μL per well) and incubated for 10-20 minutes while it is shaken at room temperature. The TMB reaction is stopped with the addition of 50 μL of stop solution (0.09 N H2SO4). The signal is quantified by measuring absorbance at 450 nm. IC50 values are determined for PF299804 using the median effect method.
Cell Research Growth and inhibition of growth is assessed by 5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay. This assay, a colorimetric method fordetermining the number of viable cells, is based on the bioreduction of MTS by cells to a formazan product that is soluble in cell culture medium, can be detected spectrophotometrically. The cells are exposed totreatment for 72 hours, and the number of cells used per experiment is determined empirically. All experimental points are set up in 6 to 12 wells, and all experiments are repeated at least thrice. The data are graphically displayed using GraphPad Prism version 3.00 for Windows (GraphPad Software). The curves are fitted using a nonlinear regression model with a sigmoidal dose response.(Only for Reference)
Synonyms PF-299804, PF-00299804, PF299
Molecular Weight 469.94
Formula C24H25ClFN5O2
CAS No. 1110813-31-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

1eq. HCl: 47 mg/mL (100 mM)

DMSO: 47 mg/mL (100 mM)

TargetMolReferences and Literature

1. Engelman JA, et al, Cancer Res, 2007, 67(24), 11924-11932. 2. Gonzales AJ, et al, Mol Cancer Ther, 2008, 7(7), 1880-1889. 3. Nam HJ, et al, Mol Cancer Ther, 2012, 11(2), 439-451. 4. Kalous O, et al, Mol Cancer Ther, 2012, Jul 3.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library Covalent Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Dacomitinib 1110813-31-4 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR PF 299 HER1 PF 00299804 PF299804 Epidermal growth factor receptor inhibit PF-299804 Inhibitor PF-00299804 PF 299804 PF-299 PF00299804 ErbB-1 PF299 inhibitor

 

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