Description
A dual inhibitor of FMS and KIT (IC50s = 28 and 16 nM, respectively); is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50s = 91 and 130 nM, respectively) in a panel of 400 kinases at 1 µM; inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC50s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells (IC50s = 380 and 230 nM, respectively); reduces TNF-α and IL-6 release in a rat model of LPS-induced cytokine release at 40 mg/kg; reduces mast cell degranulation in a mouse model of PCA; inhibits bone destruction and delays disease progression in a mouse model of CIA; reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain