Daporinad (FK866)

C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.

(E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide

0 - 10 nM

20 mg/kg

0.09 nM [1], 0.09 nM [1], 0.09 nM [1], 0.09 nM [1], 0.09 nM [1], 0.09 nM [1]

APO866 administered intraperitoneally at dose of 20 mg/kg twice a day for 4 days, repeat weekly over 3 weeks, prevents and abrogats tumor growth in C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. [1] APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA. [2]

For MTT assays, 0.5, 106 cells/mL is plated in triplicate on 96-well plates. APO866 (0.01 nM-100 nM) is added in 50 L of culture medium, with culture medium alone serving as control. After 72 or 96 hours of incubation, 15 L of dye solution is added to each well and cells are incubated for an additional 4 hours. Stop solution (100 L/well) is added for 1 hour and the absorbance is read at 570 nm on a spectrophotometer. For trypan blue dye exclusion staining, 0.5, 105 cells/well is grown in 6-well plates with 1 mL media in the absence or presence of APO866 for 96 hours. Cells from each sample are incubated with 10 L trypan blue solution (at a 1:1 ratio [vol/vol] for 1 minute). Cell survival is determined by calculating proportion of live (unstained) cells.

APO866 (FK866) Chemical Structure

2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO