Chemical Name: (2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Biological ActivityPotent, 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.
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.
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.
Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer.
Schiffer et al.
No product specific FAQs exist for this product, however you mayView all Small Molecule FAQs
Reviews for HKI 357
There are currently no reviews for this product. Be the first to review HKI 357 and earn rewards!
Have you used HKI 357?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image