HKI 357
Chemical Name: (2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Purity: ≥98%
Biological Activity
HKI 357 is a 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.Technical Data
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.
Background References
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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.
J.Med.Chem., 2005;48:1107 -
Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer.
Schiffer et al.
Mol.Pharmacol., 2007;71:508 -
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefi.
Kwak et al.
Proc.Natl.Acad.Sci.USA, 2005;102:7665
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