|IcotinibEGFR tyrosine kinase inhibitor|
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Cas No.||610798-31-7||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
Icotinib is a potent and specific EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor (IC50 = 5 nM) 
EGFR are family of receptor tyrosine kinase that is a transmembrane protein involved in the regulation of cell proliferation, motility and apoptosis. EGFR are expressed in various human cancer types, including breast, head & neck, NSCLC (non-small cell lung cancer) and ovarian caners. 
In human epidermoid carcinoma A431 cell line, Icotinib inhibited EGF-induced EGFR phosphorylation in a dose-dependent manner. Icotinib inhibited tyrosine phosphorylation of a variety of intracellular proteins. 
In different types of tumor xenograft mice models, Icotinib inhibited tumor growth in a dose-dependent manner without pronounced adverse effect in body weight loss and toxicity signs. In a randomized, double-blind, Gefitinib as control and multi-center phase III trial, Icotinib demonstrated efficacy on NSCLC in advanced stage. 
 Tan F, Shen X, Wang D, Xie G, Zhang X, Ding L, Hu Y, He W, Wang Y, Wang Y. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82.