Icotinib

Icotinib is an inhibitor of EGFR (IC₅₀ = 2 nM).¹ It is selective for EGFR over Abl, Abl2, and c-Src tyrosine kinases at 1,000 nM. Icotinib inhibits EGFR-mediated tyrosine phosphorylation in A431 human epidermoid carcinoma cells with an IC₅₀ value of 45 nM. It inhibits the growth of PC-9 and HCC827 non-small cell lung cancer (NSCLC) cells (IC₅₀s = <20 and <1,250 nM, respectively), which contain EGFR mutations, and A549 cells (IC₅₀ = 8,800 nM), which do not.² It also inhibits migration of HCC827 cells when used at a concentration of 100 nM and increases apoptosis by 43.7% at 10 nM. Icotinib reduces tumor growth in a variety of mouse xenograft models when administered at doses ranging from 50 to 120 mg/kg per day.

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1. Hu, S., Xie, G., Zhang, D.X., et al. Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors. Bioorg. Med. Chem. Lett. 22(19), 6301-6305 (2012).

2. Yang, G., Yao, Y., Zhou, J., et al. Effects of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in EGFR-mutated non-small cell lung cancer. Oncol. Rep. 27(6), 2066-2072 (2012).