FK866 (APO866, Daporinad)

Description: Daporinad (APO866; FK-866; APO-866; K 22.175) is a novel and potent inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with potential antitumor and antiangiogenic activity. It inhibits NMPRTase with an IC50 of 0.09 nM in a cell-free assay. FK866 acts by binding to and inhibiting nicotinamide phosphoribosyltransferase (NMPRTase), thus blocking the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3), which may deplete energy reserves in metabolically active tumor cells and induce tumor cell apoptosis. In addition, Daporinad may inhibit the production of vascular endothelial growth factor (VEGF) in tumor cells, leading to the inhibition of tumor angiogenesis.

References: Blood. 2009 Apr 2; 113(14):3276-86; Arthritis Rheum. 2011 Jul; 63(7):1866-77.

Related CAS #: 201034-75-5; 658084-64-1;