HKI 357

Cat. No. 3580

HKI 357 C31H29ClFN5O3 [848133-17-5]

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Chemical Name: (2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide

Biological Activity

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

M.Wt:
574.05
Formula:
C31H29ClFN5O3
Solubility:
Soluble to 100 mM in DMSO and to 25 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
848133-17-5

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Schiffer et al (2007) Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer. Mol.Pharmacol. 71 508. PMID: 16968809.

Kwak et al (2005) Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc.Natl.Acad.Sci.USA 102 7665. PMID: 15897464.

Tsou et al (2005) Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity. J.Med.Chem. 48 1107. PMID: 15715478.

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Keywords: HKI 357, supplier, HKI357, EGFR, epidermal, growth, factor, receptors, inhibitors, inhibits, irreversible, dual, potent, ErbB2, HER2, Tocris Bioscience, EGFR Inhibitor products

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