Scott Wilhelm and Du-Shieng Chien Pages 2255 - 2257 ( 3 )
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.
bay43-9006,mek-1,erk-1,raf kinase inhibitor,raf/mek/erk signaling
, Bayer Research Center, Institute for Preclinical Drug Development, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA