Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases

被引：7

作者：

Chen, Ning ^{[1
]}

Burli, Roland W. ^{[1
]}

Neira, Susana ^{[1
]}

Hungate, Randall ^{[1
]}

Zhang, Dawei ^{[1
]}

Yu, Violeta ^{[2
]}

Nguyen, Yen ^{[2
]}

Tudor, Yanyan ^{[2
]}

Plant, Matthew ^{[3
]}

Flynn, Shaun ^{[2
]}

Meagher, Kristin L. ^{[4
]}

Lee, Matthew R. ^{[4
]}

Zhang, Xuxia ^{[3
]}

Itano, Andrea ^{[3
]}

Schrag, Michael ^{[5
]}

Xu, Yang ^{[5
]}

Ng, Gordon Y. ^{[3
]}

Hu, Essa ^{[1
]}

机构：

[1] Amgen Inc, Dept Med Chem, Thousand Oaks, CA 91320 USA

[2] Amgen Inc, Dept HTS & Mol Pharmacol, Thousand Oaks, CA 91320 USA

[3] Amgen Inc, Dept Inflammat, Thousand Oaks, CA 91320 USA

[4] Amgen Inc, Dept Mol Struct, Thousand Oaks, CA 91320 USA

[5] Amgen Inc, Dept Pharmacokinet & Drug Metab, Thousand Oaks, CA 91320 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 14期

关键词：

c-kit; SCF; mast cell; inflammatory diseases;

D O I：

10.1016/j.bmcl.2008.05.089

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A potent and selective c-Kit inhibitor 20 was identified through a structure-activity relationship study. In an in vivo mouse model of mast cell activation, 20 blocked the SCF-induced histamine release with an EC(50) of 26 nM. (c) 2008 Elsevier Ltd. All rights reserved.

引用

收藏

页码：4137 / 4141

页数：5

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