Dacomitinib

• Product Name Alternative:

  PF-00299804; PF-299804

• UNSPSC Description:

  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].

• Target Antigen:

  Apoptosis; EGFR

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;JAK/STAT Signaling;Protein Tyrosine Kinase/RTK

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Dacomitinib.html

• Purity:

  99.74

• Solubility:

  DMSO : 40 mg/mL (ultrasonic)

• Smiles:

  O=C(/C=C/CN1CCCCC1)NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F

• Molecular Weight:

  469.94

• 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)

• Clinical Information:

  Launched

• CAS Number:

  1110813-31-4