Daporinad (FK866, APO866)

Catalog No.S2799

Daporinad (FK866, APO866) Chemical Structure

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.

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3 Customer Reviews

  • 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.

    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.

  • 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.

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.
Targets
NMPRTase [5]
(Cell-free assay)
0.4 nM(Ki)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SH-SY5Y cells MUTDfZRwfG:6aXRCpIF{e2G7 MlniR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhfG:2YXygZ4VtdHWuYYKgUmFFMFBrIHzleoVtNCCLQ{WwQVAvPSCwTR?= M4XLUFE6QTZzMUiz
human A2780 cells MkP4VJJwdGmoZYLheIlwdiCjc4PhfS=> MWG3NkBp NUnNdotkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NF0yKG6P M37J[lI1PDB3NEG5
human NYH cells NEnmXIFEgXSxdH;4bYPDqGG|c3H5 NUTjR2w{OyC5ZXXrdy=> NFq2O2NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPYUhiY3XscJMh[W[2ZYKgN{B4\WWtczDifUBkdG:wb3flcolkKHO3co\peoFtKGG|c3H5MEBKSzVyPUGuOUBvVQ>? MY[yN|Y4QTlzNR?=
human HepG2 cells NVHHfXU5TnWwY4Tpc44h[XO|YYm= NX;ye4pjOSCq MoP6TY5pcWKrdHnvckBw\iCQQV3QWEBqdiCqdX3hckBJ\XCJMjDj[YxteyC3c3nu[{BcOTSFXT3ubYNwfGmwYX3p[IUwWFKSUDDhd{B{fWK|dILheIUh[XO|ZYPz[YQh[XNiZn;ycYF1cW:wIH;mJHsyPEOfLX7pZ491cW6jbXnk[UBud26xboXjcIVwfGmmZTDh[pRmeiBzIHjyJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6pIHHuZYx6e2m|LDDJR|UxRTJwMjDuUS=> M2LLVVI1OTZ2MEi2
human PC3 cells NEHpWXhEgXSxdH;4bYPDqGG|c3H5 NHLuVWhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NF0{Njhibl2= MYGyOFE3PDB6Nh?=
human A431 cells NGHESZZEgXSxdH;4bYPDqGG|c3H5 MnjoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVYvOSCwTR?= M{fpU|I1OTZ2MEi2
human K562 cells MkT1R5l1d3SxeHnjxsBie3OjeR?= NFzIOFk6PiCq MnnYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC5OkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUeuNkBvVQ>? MYmyN|Y4QTlzNR?=
human MCF-7 cells NWf0e5VOS3m2b4TvfIlkyqCjc4PhfS=> M17hOVczKGh? NHzBfnhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0ZvNzDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGlEPTB;Nz60JI5O M4nTNlI1OTZ2MEi2
human HCT116 cells NGXmUVVEgXSxdH;4bYPDqGG|c3H5 NFvrcnk4OiCq MnjZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OD1zMD65JI5O MlPINlQyPjRyOE[=
human HT1080 cells NGDh[lhEgXSxdH;4bYPDqGG|c3H5 MYC2JIRigXN? MlfOR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQyODhyIHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2= Ml;oNlE{OzByMUW=
human HCT116 cells MlLkR5l1d3SxeHnjxsBie3OjeR?= NFft[WI3KGSjeYO= NIDZNYhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPiCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjF4IN88US=> MXeyNVM{ODBzNR?=
human A549 cells NWnLVHpbS3m2b4TvfIlkyqCjc4PhfS=> NG\qNI83KGSjeYO= MlG4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC2JIRigXNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNVYh|ryP M{THN|IyOzNyMEG1
human SNU638 cells MlLMR5l1d3SxeHnjxsBie3OjeR?= NFPWXWM3KGSjeYO= M4DXZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNPXTZ|ODDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOTZizszN M13lU|IyOzNyMEG1
human SKOV3 cells NX3FV2FFS3m2b4TvfIlkyqCjc4PhfS=> MmDpR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NF0zOTFibl2= MXmyOFE3PDB6Nh?=
human MCF7 cells MojNSpVv[3Srb36gZZN{[Xl? NFXTXnoyOCEQvF2= MoO4OkBl[Xm| MmDSRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDheEAyOCC3TTDh[pRmeiB4IHThfZMh[nliU2LCJIF{e2G7LDDJR|UxRTBwNkig{txO M3rYfVIyOzNyMEG1

... Click to View More Cell Line Experimental Data

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:

[1]

+ Expand
  • Cell lines: 41 hematologic malignant cell lines
  • Concentrations: 0 - 10 nM
  • 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 μL of culture medium, with culture medium alone serving as control. After 72 or 96 hours of incubation, 15 μL of dye solution is added to each well and cells are incubated for an additional 4 hours. Stop solution (100 μL/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 μL trypan blue solution (at a 1:1 ratio [vol/vol] for 1 minute). Cell survival is determined by calculating proportion of live (unstained) cells.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
  • Formulation: 0.9% saline
  • Dosages: 20 mg/kg
  • Administration: administered intraperitoneally twice a day for 4 days, repeated weekly over 3 weeks
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 78 mg/mL (199.22 mM)
DMSO Insoluble
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
45% Propylene glycol (dissolve first)+5% Tween 80+ddH2O
For best results, use promptly after mixing.
15mg/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
Formula

C24H29N3O2

CAS No. 658084-64-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00435084 Completed B-cell Chronic Lymphocytic Leukemia Onxeo February 2007 Phase 1|Phase 2
NCT00431912 Completed Cutaneous T-cell Lymphoma Onxeo February 2007 Phase 2
NCT00432107 Completed Melanoma Onxeo July 2006 Phase 2

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    We are considering the use of S2799 for in vivo injections, Any suggestions for the formula?

  • 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.

Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID