Item no. |
S2799-25 |
Manufacturer |
Selleckchem
|
CASRN |
658084-64-1 |
Amount |
25 mg |
Category |
|
Type |
Inhibitors |
Specific against |
other |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Alias |
658084-64-1' |
Similar products |
APO866 |
Available |
|
Administration |
administered intraperitoneally twice a day for 4 days, repeated weekly over 3 weeks |
Animal Models |
C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. |
Cell lines |
41 hematologic malignant cell lines |
Chemical Name |
(E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide |
Clinical Trials |
APO866 has finished phase II study in patients with B-Cell Chronic Lymphocytic Leukemia |
Concentrations |
0 - 10 nM |
Description |
APO866 effectively inhibits NAMPT with IC50 of 0.09 nM. |
Dosages |
20 mg/kg |
Formulation |
0.9% saline |
IC50 |
0.09 nM [1], 0.09 nM [1], 0.09 nM [1], 0.09 nM [1], 0.09 nM [1], 0.09 nM [1] |
In vitro |
APO866 at low concentrations ranging from 0.09-27 nM induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia [AML], acute lymphoblastic leukemia [ALL], mantle cell lymphoma [MCL], chronic lymphocytic leukemia [CLL], and T-cell lymphoma. APO866 at low concentrations ranging from 0-10 nM induces cell death, this effect is independent of caspase activation but is associated with depolarization of mitochondrial membrane. APO866 at concentrations ranging from 0-10 nM dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. [1] APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells. [2] |
In vivo |
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] |
Incubation Time |
72 hours or 96 hours |
Method |
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. |
Molecular Weight (MW) |
391, 51 |
Picture ChemicalStructure Description |
APO866 (FK866) Chemical Structure |
Solubility (25C) |
DMSO <1 mg/mL, Water <1 mg/mL, Ethanol 78 mg/mL |
Storage |
2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO |
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.