APO866 (FK866) (0.09-27 nM) induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia, acute lymphoblastic leukemia, mantle cell lymphoma, chronic lymphocytic leukemia, and T-cell lymphoma. APO866 (FK866) (0-10 nM) dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. APO866 (FK866) (10 nM) inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells. 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.
 |
Source | Int J Mol Med (2017). Figure 4. FK866 |
| Method | flow cytometry | |
| Cell Lines | Endothelial progenitor cells | |
| Concentrations | 10 μM | |
| Incubation Time | 48 h | |
| Results | Recombinant human visfatin induced a dose-dependent and significant increase in EPC apoptosis, and this effect was completely abrogated by pre-treatment with FK866. |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c nude or nonleaky C.B.-17 SCID mice (6 to 10 weeks old) |
| Formulation | in 200 uL 0.9% saline |
| Dosages | 20 mg/kg, twice a day for 4 days, repeated weekly over 3 weeks |
| Administration | intraperitoneally |
| Molecular Weight | 391.51 |
| Formula | C24H29N3O2 |
| CAS Number | 658084-64-1 |
| Solubility (25°C) | Ethanol 48 mg/mL DMSO 48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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