Daporinad (FK866, APO866)
Catalog No.S2799
Molecular Weight(MW): 391.51
Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2.
6 Customer Reviews
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Bar graph showing the effect of the PBEF inhibitor FK866 on PLB-induced autophagy in PC-3 cells. Data are presented as the mean ± SD of three independent experiments. *P<0.05; **P<0.01; and ***P<0.001 by one-way ANOVA.
Drug Des Devel Ther, 2015, 9: 1511-54. Daporinad (FK866, APO866) purchased from Selleck.
Effect of metabolic inhibitors on SRC-1 protein levels. A549 cells grown in glucose-containing medium were treated with NAM or FK866 at the indicated concentration.
Mol Endocrinol 2014 28(3), 395-405. Daporinad (FK866, APO866) purchased from Selleck.
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Paraffin-embedded tumor sections derived from MiaPaCa-2 were stained with H&E or anti-Ki67 antibodies (Scale bar: 100 μm); apoptotic cells were visualized by TUNEL staining (green) and counterstained with DAPI (blue) (Scale bar: 10 μm). The proliferation index and apoptotic index in tumor sections were also quantified. These animal experiments were repeated once (n = 5mice per treatment group).
Cancer Lett, 2016, 379(1):1-11.. Daporinad (FK866, APO866) purchased from Selleck.
Immunofluorescence analysis of Aggrecan and Collagen II expression in NP cells.
Cell Physiol Biochem, 2018, 49(6):2463-2482. Daporinad (FK866, APO866) purchased from Selleck.
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Inhibition of NAMPT enzymatic activity decreases osteoclast recruitment in the bone remodeling model. FK866‐loaded osmotic pumps were implanted 48 hr before maxillary‐molar extraction. Rats were sacrificed 4 days after tooth extraction. Osteoclast recruitment and activity were analyzed by TRAP enzymatic staining (a) and quantified (b, c and d). N.Oc/BPm: number of TRAP+ osteoclasts per mm of bone surface, Oc.S:BS (%): resorption surface, N.Nc: mean number of nuclei per osteoclast. Magnification ×200. Boxes are delimited by the first and third quartiles (Q1, Q3) and the line shows the median. Outliers are represented by the extreme values, defined as values lower then Q1—1.5 IQR (Inter Quartile Range) or higher then Q3 + 1.5 IQR. (+) represents the mean, *p ≤ 0.05, **p ≤ 0.01 by the Mann-Whitney U-test.
J Cell Physiol, 2018, 233(9):7402-7414. Daporinad (FK866, APO866) purchased from Selleck.
Western blot analysis showing that myelin basic protein (MBP) expression was higher in the NAM group compared to the other three groups at 14 d after stroke induction.
Neural Plast, 2017, 2017:7019803. Daporinad (FK866, APO866) purchased from Selleck.
Purity & Quality Control
Choose Selective Transferase Inhibitors
Biological Activity
| Description | Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| Assay |
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| 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] |
Protocol
| Cell Research: |
+ Expand
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| Animal Research: |
+ Expand
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Solubility (25°C)
| In vitro | Ethanol | 78 mg/mL (199.22 mM) |
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| DMSO | Insoluble | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O For best results, use promptly after mixing. |
4mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 391.51 |
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| Formula | C24H29N3O2 |
| CAS No. | 658084-64-1 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Molarity Calculator
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions
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Question 1:
We are considering the use of S2799 for in vivo injections, Any suggestions for the formula?
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Answer:
The vehicle we recommend for S2799 in vivo study is 45% Propylene glycol (dissolve first) +5% Tween 80+ddH2O. You can dissolve the compound in Propylene glycol first and then dilute with water with Tween 80. The solution is clear and can be used for injection.
