Daporinad (FK866, APO866)

For research use only.

Catalog No.S2799

25 publications

Daporinad (FK866, APO866) Chemical Structure

CAS No. 658084-64-1

Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.

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Selleck's Daporinad (FK866, APO866) has been cited by 25 publications

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Choose Selective Transferase Inhibitors

Biological Activity

Description Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.
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 NYHSPIV{S3m2b4TvfIlkyqCjc4PhfS=> MVfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kB1d3SjbDDj[YxtfWyjcjDORWQpWClibHX2[YwtKEmFNUC9NE42KG6P M3zkNVE6QTZzMUiz
human A2780 cells NGDNdnBRem:uaX\ldoF1cW:wIHHzd4F6 NYe4TFNoPzJiaB?= MkSzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhUUN3ME2xJI5O MmXVNlQ1ODV2MUm=
human NYH cells NYrv[oY4S3m2b4TvfIlkyqCjc4PhfS=> M1HCSlMhf2Wna4O= M3m3VmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5[UCClZXzsd{Bi\nSncjCzJJdm\Wu|IHL5JINtd26xZ3XubYMhe3W{dnn2ZYwh[XO|YYmsJGlEPTB;MT61JI5O NEK0PJEzOzZ5OUmxOS=>
human HepG2 cells MYLGeY5kfGmxbjDhd5NigQ>? M1j5c|EhcA>? NUf3dI0{UW6qaXLpeIlwdiCxZjDORW1RXCCrbjDoeY1idiCKZYDHNkBk\WyuczD1d4lv\yCdMUTDYU1vcWOxdHnuZY1q\GVxUGLQVEBieyC|dXLzeJJifGViYYPz[ZN{\WRiYYOg[o9zdWG2aX;uJI9nKFtzNFPdMY5q[2:2aX7hcYll\SCvb37vcpVkdGWxdHnk[UBi\nSncjCxJIhzKGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7nJIFv[Wy7c3nzMEBKSzVyPUKuNkBvVQ>? MUWyOFE3PDB6Nh?=
human PC3 cells NWjXXnd2S3m2b4TvfIlkyqCjc4PhfS=> NWrGT|B4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVA:Oy56IH7N MXyyOFE3PDB6Nh?=
human A431 cells M3u1VWN6fG:2b4jpZ:Kh[XO|YYm= MmDvR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVYvOSCwTR?= M{WwSFI1OTZ2MEi2
human K562 cells NGfrcmtEgXSxdH;4bYPDqGG|c3H5 Mmi3PVYhcA>? NEXoSYhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUC9O{4zKG6P NHvqTWUzOzZ5OUmxOS=>
human MCF-7 cells MX\DfZRwfG:6aXRCpIF{e2G7 NELU[FE4OiCq NV3jWGF1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOILUegZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGfTWE0yKGG|c3H5MEBKSzVyPUeuOEBvVQ>? MorWNlQyPjRyOE[=
human HCT116 cells MYXDfZRwfG:6aXRCpIF{e2G7 M3TxfVczKGh? NWDjdWc4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDXV3QuOSCjc4PhfUwhUUN3ME2xNE46KG6P NV\qVJd[OjRzNkSwPFY>
human HT1080 cells NF7aTI1EgXSxdH;4bYPDqGG|c3H5 M1zuPVYh\GG7cx?= MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWFExQDBiY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlE3KM7:TR?= NFvWSpgzOTN|MECxOS=>
human A549 cells MnPQR5l1d3SxeHnjxsBie3OjeR?= MkfvOkBl[Xm| M1;CNWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlE3KM7:TR?= NF7CT2kzOTN|MECxOS=>
human SNU638 cells MYPDfZRwfG:6aXRCpIF{e2G7 NH3KU5E3KGSjeYO= NX\v[3ZGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06XNkO4JINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVA:OC5zNjFOwG0> NYDpZ2Q3OjF|M{CwNVU>
human SKOV3 cells MoLiR5l1d3SxeHnjxsBie3OjeR?= MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVIyOSCwTR?= MXKyOFE3PDB6Nh?=
human MCF7 cells M3rzTWZ2dmO2aX;uJIF{e2G7 MmrPNVAh|ryP MXS2JIRigXN? M4\RVWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZZQhOTBidV2gZYZ1\XJiNjDkZZl{KGK7IGPSRkBie3OjeTygTWM2OD1yLk[4JO69VQ>? Mln0NlE{OzByMUW=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot

PubMed: 29905535     

Human retinal pigment epithelial cells (ARPE-19) were treated with different doses (0.01-10μM) of FK866 and expression of SIRT1 was evaluated by western blotting.

p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1; 

PubMed: 29541451     

CEM PA cells were treated with 5 and 100 nM FK866 for 48 h. Western blot showing expression of AMPK, mTOR, 4EBP1, and EIF2A in CEM PA cells.

AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448); 

PubMed: 26542945     

Jurkat cells were treated for 48 h with or without (Mock) the indicated concentration of FK866. Thereafter, cells were lysed and the levels of total and p-Akt (Ser-473), total and p-MTOR (Ser-2448), total and p-4EBP1 (Ser-65 and Thr-70).

29905535 29541451 26542945

PubMed: 29996103     

Immunofluorescence for pMLKL (monoclonal pMLKL antibody, red, phospho S358) and nuclei (DAPI, blue) in THP-1 cells treated with the indicated concentrations of FK866 for 6 hr. Scale bars, 10 μm. 


PubMed: 22207684     

Representative DUOLINK images of phospho-GSK3β (Ser9) protein expression in HL60 cells treated with 10 nM of FK866 for 96 h or 100 nM of AC93253 for 48 h, or with DMSO as a control.

ph-β-catenin ; 

PubMed: 22207684     

Representative images of inactive phospho-β-catenin (Ser33/37) protein expression in HL60 cells treated with 10 nM of FK866, 100 nM of AC93253 or DMSO as a control

29996103 22207684
Growth inhibition assay
Cell viability ; 

PubMed: 27462772     

Twenty-three PDAC-derived PCCs were treated for 72 h with increasing concentrations of FK866 ranging from 0 to 1000 nM. The horizontal dotted line indicates 50% cell viability. PCCs with the highest sensitivity are highlighted by a blue line and those wit䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ

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]


Cell Research:


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  • 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:


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  • Animal Models: C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
  • 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 DMSO Insoluble
Water Insoluble
Ethanol '78 mg/mL
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.

* 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


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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00435084 Completed Drug: APO866 B-cell Chronic Lymphocytic Leukemia Onxeo February 2007 Phase 1|Phase 2

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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