Pelitinib
Chemical Name: (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Purity: ≥97%
Biological Activity
Pelitinib is a potent irreversible EGFR inhibitor (IC50 = 20-80 nM). Selective for EGFR over Src, MEK/ERK, erbB2, Raf, c-Met and Cdk4 (IC50 values are 282, 800, 1255, 3353, 4100 and >20,000). Inhibits the growth of tumors overexpressing EGFR in vivo. Orally bioavailable.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.
Additional Information
Background References
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Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: Implications for the emergence and reversal of cancer drug resistance
Hegedüs
Biochem. Pharmacol., 2012;84:260 -
Blocking airway mucous cell metaplasia by inhibiting EGFR antiapoptosis and IL-13 transdifferentiation signals.
Tyner et al.
J.Clin.Invest., 2006;116:309 -
Combinatorial chemoprevention of intestinal neoplasia.
Torrance et al.
Nat.Med., 2000;6:1024 -
Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human
Nunes et al.
Mol.Cancer Ther., 2004;3:21
Product Datasheets
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