FK-866

• CAT Number: I004482
• CAS Number: 658084-64-1
• Molecular Formula: C₂₄H₂₉N₃O₂
• Molecular Weight: 391.51
• Purity: ≥95%
• Target: Transferase
• Solubility: DMSO: 25 mg/mL
• Storage: 3 years -20C powder
• IC50: 0.09 nM
• InChI: InChI=1S/C24H29N3O2/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28)/b12-11+
• InChIKey: KPBNHDGDUADAGP-VAWYXSNFSA-N
• SMILES: C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3

FK866(APO866; Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM.IC50 value: 0.09 nMTarget: NMPRTaseFK866 inhibits nicotinamide phosphoribosyltransferase (NMPRTase), a key enzyme involved in nicotinamide adenine dinucleotide (NAD) biosynthesis from the natural precursor nicotinamide. FK866 triggered cytotoxicity in multiple myeloma (MM) cell lines and patient MM cells, but not normal donor as well as MM patients PBMCs. Importantly, FK866 in a dose-dependent fashion triggered cytotoxicity in MM cells resistant to conventional and novel anti-MM therapies and overcomes the protective effects of cytokines (IL-6, IGF-1) and bone marrow stromal cells. FK866 demonstrated significant anti-MM activity in a xenograft-murine MM model, associated with down-regulation of ERK1/2 phosphorylation and proteolytic cleavage of LC3 in tumor cells.

Reference

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[5]. Aimable Nahimana, Antoine Attinger, Dominique Aubry, et al. The NAD biosynthesis inhibitor APO866 has potent antitumor activity against hematologic malignancies. Blood April 2, 2009 ,113 (14): 3276-3286
[6]. Mun-Kyoung Kim, Jun Hyuck Lee, Hun Kim, et al. Crystal Structure of Visfatin/Pre-B Cell Colony-enhancing Factor 1/Nicotinamide Phosphoribosyltransferase, Free and in Complex with the Anti-cancer Agent FK-866. Journal of Molecular Biology. 2006,362（1）：66-77