期刊
FUTURE MEDICINAL CHEMISTRY
卷 1, 期 6, 页码 1153-1171出版社
FUTURE SCI LTD
DOI: 10.4155/FMC.09.89
关键词
-
资金
- OSI Pharmaceuticals, Inc
Background: The IGF-I receptor (IGF-IR) has been implicated in the promotion of tumorigenesis, metastasis and resistance to cancer therapies. Therefore, this receptor has become a major focus for the development of anticancer agents. Results: Our lead optimization efforts that blended structure-based design and empirical medicinal chemistry led to the discovery of OSI-906, a novel small-molecule dual IGF-IR/insulin receptor (IR) kinase inhibitor. OSI-906 potently and selectively inhibits autophosphorylation of both human IGF-IR and IR, displays in vitro antiproliferative effects in a variety of tumor cell lines and shows robust in vivo anti-tumor efficacy in an IGF-I R-driven xenograft model when administered orally once daily. Conclusion: OSI-906 is a novel, potent, selective and orally bioavailable dual IGF-IR/IR kinase inhibitor with favorable preclinical drug-like properties, which has demonstrated in vivo efficacy in tumor models and is currently in clinical testing.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据