Daporinad (FK866, APO866)

For research use only.

Catalog No.S2799

25 publications

Daporinad (FK866, APO866) Chemical Structure

Molecular Weight(MW): 391.51

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

Size Price Stock Quantity  
USD 90 In stock
USD 170 In stock
USD 370 In stock
USD 570 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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

Purity & Quality Control

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. 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 NV\rWGV[S3m2b4TvfIlkyqCjc4PhfS=> NH36SHNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iC2b4ThcEBk\WyudXzhdkBPSURqUDmgcIV3\WxuIFnDOVA:OC53IH7N M1O3dVE6QTZzMUiz
human A2780 cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 NEfpU404OiCq MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy|IHHmeIVzKDd{IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBKSzVyPUGgcm0> MWKyOFQxPTRzOR?=
human NYH cells M2PTXWN6fG:2b4jpZ:Kh[XO|YYm= NIDsSYQ{KHenZXvz M1GyOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5[UCClZXzsd{Bi\nSncjCzJJdm\Wu|IHL5JINtd26xZ3XubYMhe3W{dnn2ZYwh[XO|YYmsJGlEPTB;MT61JI5O NInIWY4zOzZ5OUmxOS=>
human HepG2 cells MmDHSpVv[3Srb36gZZN{[Xl? MVixJIg> MlP2TY5pcWKrdHnvckBw\iCQQV3QWEBqdiCqdX3hckBJ\XCJMjDj[YxteyC3c3nu[{BcOTSFXT3ubYNwfGmwYX3p[IUwWFKSUDDhd{B{fWK|dILheIUh[XO|ZYPz[YQh[XNiZn;ycYF1cW:wIH;mJHsyPEOfLX7pZ491cW6jbXnk[UBud26xboXjcIVwfGmmZTDh[pRmeiBzIHjyJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6pIHHuZYx6e2m|LDDJR|UxRTJwMjDuUS=> NWXSRoN[OjRzNkSwPFY>
human PC3 cells MXzDfZRwfG:6aXRCpIF{e2G7 MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3ME2zMlghdk1? MoHiNlQyPjRyOE[=
human A431 cells NGLETo5EgXSxdH;4bYPDqGG|c3H5 NI\nUYpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVA:Pi5zIH7N NFy2VXUzPDF4NEC4Oi=>
human K562 cells M1zrO2N6fG:2b4jpZ:Kh[XO|YYm= NGHYTYc6PiCq NHnHPXZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUC9O{4zKG6P NWm1c5hCOjN4N{m5NVU>
human MCF-7 cells MmrQR5l1d3SxeHnjxsBie3OjeR?= M4PTdFczKGh? NV;uSpRPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOILUegZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGfTWE0yKGG|c3H5MEBKSzVyPUeuOEBvVQ>? Mnv1NlQyPjRyOE[=
human HCT116 cells NHza[GpEgXSxdH;4bYPDqGG|c3H5 NEfCV3c4OiCq M17aOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGlEPTB;MUCuPUBvVQ>? NETycG8zPDF4NEC4Oi=>
human HT1080 cells NVn6OHNzS3m2b4TvfIlkyqCjc4PhfS=> NHnuW5g3KGSjeYO= NXzCe5ZPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRzMEiwJINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVA:OC5zNjFOwG0> MmrCNlE{OzByMUW=
human HCT116 cells NWnIWoo{S3m2b4TvfIlkyqCjc4PhfS=> MX:2JIRigXN? MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlE3KM7:TR?= Ml[3NlE{OzByMUW=
human A549 cells MUfDfZRwfG:6aXRCpIF{e2G7 NUCyXFEzPiCmYYnz NGDVRZJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2= MlvONlE{OzByMUW=
human SNU638 cells M2W5XmN6fG:2b4jpZ:Kh[XO|YYm= M3znOlYh\GG7cx?= Ml\XR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25WPjN6IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2= MkTrNlE{OzByMUW=
human SKOV3 cells NFXCZWxEgXSxdH;4bYPDqGG|c3H5 MoDzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NF0zOTFibl2= NXLBRoVbOjRzNkSwPFY>
human MCF7 cells NXHjdoVYTnWwY4Tpc44h[XO|YYm= MlLPNVAh|ryP MkPHOkBl[Xm| Mn;iRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDheEAyOCC3TTDh[pRmeiB4IHThfZMh[nliU2LCJIF{e2G7LDDJR|UxRTBwNkig{txO MkTQNlE{OzByMUW=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
SIRT1; 

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
Immunofluorescence
pMLKL; 

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. 

phGSK3β; 

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

27462772
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]

- Collapse
  • 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]

- Collapse
  • 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 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):
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
Formula

C24H29N3O2

CAS No. 658084-64-1
Storage powder
in solvent
Synonyms N/A
Smiles O=C(NCCCCC1CCN(CC1)C(=O)C2=CC=CC=C2)/C=C/C3=CC=CN=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

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)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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

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 )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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

Tags: buy Daporinad (FK866, APO866) | Daporinad (FK866, APO866) supplier | purchase Daporinad (FK866, APO866) | Daporinad (FK866, APO866) cost | Daporinad (FK866, APO866) manufacturer | order Daporinad (FK866, APO866) | Daporinad (FK866, APO866) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID