ArtNr |
S2799-10mM/1mL |
Hersteller |
Selleckchem
|
CAS-Nr. |
658084-64-1 |
Menge |
10 mM/1 ml |
Kategorie |
|
Typ |
Inhibitors |
Specific against |
other |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Lieferbar |
|
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 |
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