Potent, irreversible inhibitor of ErbB2 (HER2) and EGFR (IC50
values are 33 and 34 nM respectively). Suppresses ligand-induced EGFR autophosphorylation and cell proliferation in NCI-H1975 cells containing L858R and T790M mutations. Circumvents mechanisms of resistance to Iressa
(Cat. No. 3000) in non-small-cell lung cancer cells.
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All Tocris products are intended for laboratory research use only.
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.
Kwak et al.
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
Tsou et al.
Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer.
Schiffer et al.