GW-2580 (870483-87-7) is a potent and selective inhibitor of cFMS receptor kinase. Completely inhibits cFMS in vitro at 60 nM with no activity against 26 other kinases1. Completely inhibits CSF-1 induced growth of mouse M-NFS-60 myeloid cells and human monocytes (at 1 μM)1. GW-2580 completely inhibits bone degradation in human osteoclasts, rat calvaria and fetal long bone1. Inhibits LPS-induced TNF production in mice. GW-2580 abrogates infiltration of macrophages into synovial joints of arthritic mice2. Active in vivo.
1) Conway et al. (2005), Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580; Proc. Natl. Acad. Sci. USA, 102 16078
2) Paniagua et al. (2010), c-Fms-mediated differentiation and priming of monocyte lineage cells play a central role in autoimmune arthritis; Arthritis Res. Ther., 12 R32