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Tocris Bioscience™ Afatinib Dimaleate
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Catalog No. 681210
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68-121-0 10 mg
68-125-0 50 mg
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Catalog No. 68-121-0 Supplier Tocris Bioscience™ Supplier No. 6812/10
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Potent dual specificity EGFR/HER2 inhibitor; active in vivo

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.

Specifications

Chemical Name or Material (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate
CAS 850140-73-7
Synonym BIBW2992
Quantity 10 mg
Molecular Formula C24H25ClFN5O3.2C4H4O4
Formula Weight 718.08
Purity 98%
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