Chemical Name: (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Biological ActivityPotent irreversible EGFR inhibitor (IC50 = 20-80 nM). Selective for EGFR over Src, MEK/ERK, erbB2, Raf, c-Met and Cdk4 (IC50 values are 282, 800, 1255, 3353, 4100 and >20,000). Inhibits the growth of tumors overexpressing EGFR in vivo. Orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human
Nunes et al.
Mol.Cancer Ther., 2004;3:21
Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: Implications for the emergence and reversal of cancer drug resistance
Biochem. Pharmacol., 2012;84:260
Blocking airway mucous cell metaplasia by inhibiting EGFR antiapoptosis and IL-13 transdifferentiation signals.
Tyner et al.
Combinatorial chemoprevention of intestinal neoplasia.
Torrance et al.
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