Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
信号通路
JAK/STAT; Protein Tyrosine Kinase
靶点
EGFR and EGFR mutants
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IC50
5nM
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体外研究
Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50value of 5nM and complete inhibition at 62.5nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in our proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, we found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR.
体内研究
In vivo studies demonstrated that Icotinib exhibited potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug was well tolerated at doses up to 120mg/kg/day in mice without mortality or significant body weight loss during the treatment. A head to head randomized, double blind phase III trial using Gefitinib as an active control for patients with advanced non-small cell lung cancer (NSCLC) was finished recently (Trial registration ID: NCT01040780).
临床实验
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相关实验数据(此数据来自于公开文献,联迈生物并不保证其有效性):
酶活性检测实验
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细胞实验
细胞系
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动物实验
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配制
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给药方式
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参考文献: 1. Tan F, et al. Lung Cancer. 2012 May, 76(2), 177-82. 包装清单: