FK 866 hydrochloride is an inhibitor of nicotinamide phosphoribosyltransferase (IC50: 0.09nM and 27.2nM).

In the vitro MTT assay using a panel of 41 human hematologic cancer cell lines, most cancer cells are sensitive to low concentrations of FK866. Among these cancer cells, AML cells are the most sensitive. FK866 is shown selective to human hematologic malignant cells and the normal human HPCs are resistant to FK866 treatment. It is found that FK866 induces cell death in a caspase-independent pathway but in a dose-dependent manner to induce mitochondrial membrane depolarization. Additionally, FK866 induces cell autophagy dependent on de novo protein synthesis. FK866 also reduces ATP levels in ML-2 cells due to the inhibition of NAD synthesis.

The antitumor efficacy of FK866 is also shown in the in vivo models. FK866 significantly prevents tumor growth both in mice xenografted subcutaneously with AML-M4 and Namalwa cells. Furthermore, FK866 clears tumor cells to below detectable levels and results in 80% survival for the long-term [1].

T22785

C24H30ClN3O2

427.97

FK 866 hydrochloride;FK 866 hydrochloride (658084-64-1 free base)

DMSO:≥18.95mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years