HKI 357

Discontinued Product

HKI 357 (Cat. No. 3580) has been withdrawn from sale for commercial reasons.
Description: Dual irreversible inhibitor of ErbB2 and EGFR
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% (HPLC)
Literature (1)

Biological Activity for HKI 357

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 for HKI 357

M. Wt 574.05
Formula C31H29ClFN5O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 848133-17-5
PubChem ID 11238512
Smiles O=C(/C=C/CN(C)C)NC1=C(OCC)C=C(N=CC(C#N)=C2NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1

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.

Product Datasheets for HKI 357

Certificate of Analysis / Product Datasheet
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References for HKI 357

References are publications that support the biological activity of the product.

Kwak et al (2005) Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefi. 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

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

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Citations for HKI 357

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Literature in this Area

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