Login Register Cart 0
Generic placeholder image

Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Back
Journal Home About Journal Editorial Board Journal Insight Current Issue Volumes/Issues
Subscribe

BAY 43-9006: Preclinical Data

Author(s): Scott Wilhelm and Du-Shieng Chien

Volume 8, Issue 25, 2002

Page: [2255 - 2257] Pages: 3

DOI: 10.2174/1381612023393026

Price: $65

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

« Previous Next »

Rights & Permissions Print Cite
Article Metrics
78
© 2025 Bentham Science Publishers | Privacy Policy