Chemical Name: (2E)-N-[4-[[3-Chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Biological ActivityNeratinib is a potent, irreversible inhibitor of HER-2/ErbB2 receptor tyrosine kinase and EGFR kinase (IC50 = 59 nM and 92 nM, respectively). Neratinib reduces receptor autophosphorylation and proliferation of EGFR-dependent cancer cells, blocks cell-cycle progression and inhibits HER-2 signaling pathways. Neratinib suppresses proliferation of gefitinib-resistant non-small cell lung cancer cells expressing mutant EGFR. Also inhibits MST1 (IC50 = 37.7 nM). Orally bioavailable.
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.
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.
Kwak et al.
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