Ki20227 is an inhibitor of macrophage colony stimulating factor 1 (CSF1) receptor tyrosine kinase (c-Fms; IC50 = 2 nM). It inhibits CSF1-dependent c-Fms phosphorylation in a dose-dependent manner in RAW264.7 cells and reduces CSF1-dependent growth of M-NFS-60 cells (IC50 = 14 nM). Ki20227 suppresses development of TRAP-positive osteoclast-like cells from murine bone marrow (IC50 = 40 nM) and decreases the number and area of osteolytic lesions on femurs and tibiae in a murine A375 subcutaneous xenograft model. Ki20227 also reduces TNF-α infiltration and osteolytic bone destruction in a collagen-induced arthritis (CIA) mouse model.