Afatinib dimaleate

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Afatinib dimaleate | CAS No. 850140-73-7 | EGF Receptor Inhibitors
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Description: Potent dual specificity EGFR/HER2 inhibitor; active in vivo
Alternative Names: BIBW2992

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%

Product Details
Citations (1)

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

Soluble to 20 mM in water with gentle warming and to 50 mM in DMSO
Store at -20°C

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.

Product Datasheets

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Citation for Afatinib dimaleate

The citations listed below are publications that use Tocris products. Selected citations for Afatinib dimaleate include:

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