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:

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

Reference:

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.