Dacomitinib
Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].
Product Specifications
CAS Number
1110813-31-4
Product Name Alternative
PF-00299804; PF-299804
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; EGFR
Type
Reference compound
Related Pathways
Apoptosis; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Dacomitinib.html
Purity
99.74
Solubility
DMSO : 38.89 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=C(/C=C/CN1CCCCC1)NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F
Molecular Formula
C24H25ClFN5O2
Molecular Weight
469.94
Precautions
H302, H315, H319, H335
References & Citations
[1]Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to ZD1839. Cancer Res. 2007 Dec 15;67 (24) :11924-32.|[2]Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to Anti-Human HER2 and GW572016. Mol Cancer Ther. 2012 Sep;11 (9) :1978-87.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
EGFR/ErbB1/HER1; ErbB2/HER2; ErbB4/HER4
Available Sizes
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