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Afatinib

Afatinib : Covalent inhibitor of EGFR and ERBB2

Structure

Information

  • EGFR
  • ERBB2
  • Covalent Inhibitor
  • Up to 100 nM

In Vitro Validations

Uniprot ID: P00533
Target Class: Kinase
Target SubClass: RTK
Potency: IC50
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

Off-Target Selectivity Assesments

Potency end-point : IC50 LYN 736 nM
Probe Selectivity in Vitro:
Afatinib was assessed against 52 off-target kinases, and it was most potent against LYN.
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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP 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

SERP 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. 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

SERP 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 )