Afatinib

ATP-competitive inhibitor, covalent inhibitor of EGFR, ERBB2

Structure

Information

Protein target names: EGFR ERBB2

Mechanism of action: ATP-competitive inhibitor, covalent inhibitor

Primary References:

In Vitro Validations

Uniprot ID: P00533
Target Class: Kinase
Target SubClass: RTK
Potency: IC 50
Potency Value: 0.5 nM
Potency Assay: In vitro kinase assays
PDB ID for probe-target interaction (3D structure): 4G5J
Target aliases:
Epidermal growth factor receptor, HER1, ERBB1, ERB ...

DOI Reference: 10.1038/onc.2008.109

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

Comments:

Treat the quoted biochemical potency with caution as it is an irreversible inhibitor. Afatinib hits wild-type and activating-mutant forms of EGFR with similar potency.

(last updated: 20 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

Potent irreversible inhibitor of EGFR and HER2. Some selectivity data are reported - ideally, a full kinase profile would be required to better understand higher dose range limit.

(last updated: 20 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

As a probe for ERBB2 this would not be recommended as it exhibits greater potency for EGFR, more suitable selective probes for ERBB2 exist. Treat the quoted biochemical potency with caution as it is an irreversible inhibitor. Hits WT and activating mutant forms of EGFR with similar potency.

(last updated: 24 May 2016 )