Current Pharmaceutical Design

William A. Banks  
VAPSHCS/GRECC S-182
Building 1, Room 810A
1600 S. Columbian Way
Seattle, WA 98108
USA

Back

BAY 43-9006: Preclinical Data

Author(s): Scott Wilhelm, Du-Shieng Chien.

Abstract:

The drug design and discovery efforts described in the previous section led to the development of a novel, small molecule Raf-1 kinase inhibitor, BAY 43-9006, which belongs to a class that can be broadly described as bis-aryl ureas (Figure 1) [1]. BAY 43-9006 was identified during a large medicinal chemistry optimization program, and this compound was selected for further pharmacological characterization based on its potent inhibition of Raf-1 (IC50 12 nM) and its favorable kinase selectivity profile [2, 3]. In vitro and in vivo experiments were designed to demonstrate effective blockade of the Raf / MEK / ERK signaling pathway in tumor cells and for anti-tumor efficacy in human xenograft models.

Keywords: bay43-9006, mek-1, erk-1, raf kinase inhibitor, raf/mek/erk signaling

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 8
ISSUE: 25
Year: 2002
Page: [2255 - 2257]
Pages: 3
DOI: 10.2174/1381612023393026
Price: $58