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Description of GW2580: GW2580 is an orally bioavailable inhibitor of cFMS kinase. GW2580 was found to completely inhibit human cFMS kinase in vitro at 0.06 microM and was inactive against 26 other kinases. GW2580 at 1 microM completely inhibited CSF-1-induced growth of mouse M-NFS-60 myeloid cells and human monocytes and completely inhibited bone degradation in cultures of human osteoclasts, rat calvaria, and rat fetal long bone. In contrast, GW2580 did not affect the growth of mouse NS0 lymphoblastoid cells, human endothelial cells, human fibroblasts, or five human tumor cell lines. GW2580 also did not affect lipopolysaccharide (LPS)-induced TNF, IL-6, and prostaglandin E2 production in freshly isolated human monocytes and mouse macrophages. After oral administration, GW2580 blocked the ability of exogenous CSF-1 to increase LPS-induced IL-6 production in mice, inhibited the growth of CSF-1-dependent M-NFS-60 tumor cells in the peritoneal cavity, and diminished the accumulation of macrophages in the peritoneal cavity after thioglycolate injection. Unexpectedly, GW2580 inhibited LPS-induced TNF production in mice, in contrast to effects on monocytes and macrophages in vitro. In conclusion, GW2580's selective inhibition of monocyte growth and bone degradation is consistent with cFMS kinase inhibition. The ability of GW2580 to chronically inhibit CSF-1 signaling through cFMS kinase in normal and tumor cells in vivo makes GW2580 a useful tool in assessing the role of cFMS kinase in normal and disease processes. [Proc Natl Acad Sci U S A. 2005 Nov 1;102(44):16078-83. Epub 2005 Oct 25.]
For the detailed information about the solubility of GW2580 (GW 2580) in water, the solubility of GW2580 (GW 2580) in DMSO, the solubility of GW2580 (GW 2580) in PBS buffer, the animal experiment（test） of GW2580 (GW 2580),the in vivo,in vitro and clinical trial test of GW2580 (GW 2580),the cell experiment（test） of GW2580 (GW 2580),the IC50, EC50 and Affinity of GW2580 (GW 2580), please contact DC Chemicals. |
