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