Afatinib dimaleate
Chemical Name: (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate
Purity: ≥98%
Biological Activity
Afatinib dimaleate is a potent dual specificity EGFR/HER2 inhibitor (IC50 are 0.4, 0.5, 10, 14, 1 nM for EGFRL858R, EGFRwt, EGFR L858R/T790M, ErbB2 (HER2) and ErbB4 (HER4), respectively). 100-fold more active than Gefitinib in L858R-T790M EGFR double mutant cell line. Irreversibly binds EGFR and HER2. Suppresses the kinase activity of wild-type and activated EGFR and HER2 mutants, including erlotinib-resistant isoforms. Induces tumor regression in xenograft and transgenic lung cancer models.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.
Li et al.
Oncogene, 2008;27:4702
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Citation for Afatinib dimaleate
The citations listed below are publications that use Tocris products. Selected citations for Afatinib dimaleate include:
1 Citation: Showing 1 - 1
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Intranasal delivery of a small-molecule ErbB inhibitor promotes recovery from acute and late-stage CNS inflammation.
Authors: Jürgen Et al.
JCI Insight 2022;7
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