Dacomitinib - PF-00299804

Based on 20 reference(s) in Google Scholar 80 100 20

Axon 3235

CAS [1110813-31-4]

MF C24H25ClFN5O2
MW 469.94

Purity: 100%
Soluble in 0.1N HCl(aq) and DMSO

Dacomitinib

Description

Dacomitinib is a potent irreversible pan-ERBB inhibitor with IC50 values of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively. Dacomitinib is a potent inhibitor of EGFR-activating mutations as well as the EGFR T790M resistance mutation both in vitro and in vivo. Additionally, Dacomitinib is a highly effective inhibitor of both the wild-type ERBB2 and the gefitinib-resistant oncogenic ERBB2 mutation identified in lung cancers.

JA Engelman et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res. 2007 Dec 15;67(24):11924-32.

JB Smaill. Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. J Med Chem. 2016 Sep 8;59(17):8103-24.

Apoptosis Cell Cycle Regulation Cell Signaling & Oncology EGFR ErbB2-HER2 JAK-STAT RTK class I; EC 2.7.10.1

Potent irreversible pan-HER inhibitor

Chemical name

(E)-N-(4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl)-4-(piperidin-1-yl)but-2-enamide

Parent CAS No.

[1110813-31-4]

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Dacomitinib - PF-00299804

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Dacomitinib - PF-00299804

Description

Chemical name

Parent CAS No.

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