FK866 (APO866) is a competitive inhibitor of pre-B cell colony-enhancing factor (PBEF), also known as nicotinamide phosphoribosyltransferase (NAMPT), by inhibiting binding of its natural substrate, nicotinamide. In MMP-3 assays, the IC50 of FK866 in the presence of 50 ng/mL NAMPT was found to be between 0.1 nM and 1 nM. When increasing the concentration of NAMPT to 200 ng/mL, the IC50 of FK866 also increased to between 10 and 100 nM. [1]
FK866 has shown to selectively induce cytotoxicity in hematologic malignant cells, but not normal hematopoetic progenitor cells. Furthermore, FK866 induces intracellular NAD and ATP depletion in hematologic tumor cells. [2]
FK866 has shown anti-inflammatory effects [1] in addition to its application in oncology. In order to increase its therapeutic effect, it was found that co-treatment with nicotinic acid can widen the safety window when compared to FK866 alone. [3]
Technical information:
| Chemical Formula: | C24H29N3O2 | |
| CAS #: | 658084-64-1 | |
| Molecular Weight: | 391.51 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | (E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide | |
| Solubility: | Up to 20 mM in DMSO | |
| Synonyms: | FK866, FK-866, APO866, Daporinad |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Evans et al., Suppression of Leukocyte Infiltration and Cartilage Degradation by Selective Inhibition of Pre-B Cell Colony-Enhancing Factor/Visfatin/Nicotinamide Phosphoribosyltransferase. Arthritis Rheum. 2011, 63(7), 1866-1877. Pubmed ID: 21400478 |
| 2. | Nahimana et al., The NAD biosynthesis inhibitor APO866 has potent antitumor efficacy against hematologic malignancies. Blood 2009, 113, 3276-3286. Pubmed ID: 19196867 |
| 3. | Olesen et al., A Preclinical Study on the Rescue of Normal Tissue by Nicotinic Acid in High-Dose Treatment with APO866, a Specific Nictoniamide Phosphoribosyltransferase Inhibitor. Mol. Cancer. Ther. 2010, 9, 1609-1617. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
