BAY 43-9006: Preclinical Data

Title: BAY 43-9006: Preclinical Data

Volume: 8 Issue: 25

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

Affiliation:

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

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.

Cite this article as:

Wilhelm Scott and Chien Du-Shieng, BAY 43-9006: Preclinical Data, Current Pharmaceutical Design 2002; 8 (25) . https://dx.doi.org/10.2174/1381612023393026