Ki-20227

Ki-20227 is an orally active, potent, and selective small molecule inhibitor of the c-Fms tyrosine kinase (also known as colony-stimulating factor 1 receptor, or CSF1R). Originally developed by Kirin Brewery (now Kyowa Kirin), Ki-20227 selectively blocks CSF1R phosphorylation and downstream signaling, thereby suppressing the differentiation and survival of osteoclasts and macrophages. In preclinical studies, it has demonstrated significant efficacy in animal models of bone metastasis, rheumatoid arthritis (collagen-induced arthritis), and multiple sclerosis (experimental autoimmune encephalomyelitis) by reducing osteolytic bone destruction, inflammatory cell infiltration, and microglial density. Ki-20227 remains in the preclinical stage of development.

Other names

1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]ureaN-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]ureaN-{4-[(6,7-dimethoxy-4-quinolyl)oxy]-2-methoxyphenyl}-N'-[1-(1,3-thiazole-2-yl)ethyl]urea