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Cellagen Technology
PBEF/NAMPT inhibitor
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]
Cellagen Technology
PBEF/NAMPT inhibitor
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]
