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.