JNJ-28312141 is a potent, orally active CSF-1 receptor (CSF-1R) kinase inhibitor with IC50 of 0.69 nM.
JNJ-28312141 shows narrow kinase selectivity profile, also potently inhibits KIT (IC50=5 nM), AXL (12 nM), TRKA (15 nM), FLT3 (30 nM), and LCK (88 nM).
JNJ-28312141 inhibits CSF-1-induced CSF-1R phosphorylation with IC50 of 5 nM, inhibits CSF-1-dependent proliferation of mouse macrophages and CSF-1-induced expression of MCP-1 by human monocytes with IC50 of 3 nM.
JNJ-28312141 inhibits the ITD-FLT3-dependent proliferation of MV-4-11 cells with IC50 of 21 nM, inhibits FLT3 ligand-induced FLT3 phosphorylation in recombinant Baf3 cells with IC50 of 76 nM.
JNJ-28312141 demonstrates potential therapeutic activity in AML, solid tumors and bone metastases in vivo.
