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.

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.

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 [1]
(Cell-free assay)
0.09 nM
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 M1LXPGN6fG:2b4jpZ:Kh[XO|YYm= NXPSTFVuS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0hvU2m1XUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZidH;0ZYwh[2WubIXsZZIhVkGGKGCpJIxmfmWuLDDJR|UxRTBwNTDuUS=> NYixUXdxOTl7NkGxPFM>
human A2780 cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 NH;IZ|M4OiCq NFfQUW1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwQVEhdk1? M{CwVlI1PDB3NEG5
human NYH cells NV3pOZBVS3m2b4TvfIlkyqCjc4PhfS=> MnzPN{B4\WWtcx?= NGTGeppEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPYUhiY3XscJMh[W[2ZYKgN{B4\WWtczDifUBkdG:wb3flcolkKHO3co\peoFtKGG|c3H5MEBKSzVyPUGuOUBvVQ>? M3nYfVI{Pjd7OUG1
human HepG2 cells M1jJdWZ2dmO2aX;uJIF{e2G7 MXixJIg> MULJcohq[mm2aX;uJI9nKE6DTWDUJIlvKGi3bXHuJGhmeEd{IHPlcIx{KHW|aX7nJHsyPEOfLX7pZ491cW6jbXnk[U9RWlCSIHHzJJN2[nO2cnH0[UBie3Onc4Pl[EBieyCob4LtZZRqd25ib3[gX|E1S11vbnnjc5RqdmGvaXTlJI1wdm:wdXPs[Y91cWSnIHHmeIVzKDFiaIKgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmdiYX7hcJl{cXNuIFnDOVA:Oi5{IH7N MX6yOFE3PDB6Nh?=
human PC3 cells NXr0VYlzS3m2b4TvfIlkyqCjc4PhfS=> NHjuXYhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NF0{Njhibl2= MnLUNlQyPjRyOE[=
human A431 cells MmLNR5l1d3SxeHnjxsBie3OjeR?= M1\BSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMh[nliY3zvco9o\W6rYzDhd5NigSxiSVO1NF03NjFibl2= NHz1d5czPDF4NEC4Oi=>
human K562 cells MYLDfZRwfG:6aXRCpIF{e2G7 MXi5OkBp NWDye3B3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVcvOiCwTR?= MX[yN|Y4QTlzNR?=
human MCF-7 cells MX3DfZRwfG:6aXRCpIF{e2G7 NYnBbnozPzJiaB?= M2WyOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETi15IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OD15LkSgcm0> MnLMNlQyPjRyOE[=
human HCT116 cells NYLrW3RsS3m2b4TvfIlkyqCjc4PhfS=> MVe3NkBp MlLiR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OD1zMD65JI5O NGTON2MzPDF4NEC4Oi=>
human HT1080 cells NF7aeJVEgXSxdH;4bYPDqGG|c3H5 MkTnOkBl[Xm| Mk\BR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQyODhyIHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2= M3:1SlIyOzNyMEG1
human HCT116 cells MlPCR5l1d3SxeHnjxsBie3OjeR?= MUW2JIRigXN? NEHtZ4xEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPiCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjF4IN88US=> M1\SNVIyOzNyMEG1
human A549 cells M{Hib2N6fG:2b4jpZ:Kh[XO|YYm= MoDLOkBl[Xm| NITvZWVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2= NV33fIJMOjF|M{CwNVU>
human SNU638 cells MX3DfZRwfG:6aXRCpIF{e2G7 NGjEOlc3KGSjeYO= NXvVbY9lS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06XNkO4JINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVA:OC5zNjFOwG0> NVmwO2QyOjF|M{CwNVU>
human SKOV3 cells NGG2XWdEgXSxdH;4bYPDqGG|c3H5 NGnMb2REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTJzMTDuUS=> MnjxNlQyPjRyOE[=
human MCF7 cells MnvLSpVv[3Srb36gZZN{[Xl? M2fBUlExKM7:TR?= MoHJOkBl[Xm| MU\BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHH0JFExKHWPIHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVA:OC54ODFOwG0> M4rYbFIyOzNyMEG1

... 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 individually and in order:
45% Propylene glycol (dissolve first)+5% Tween 80+ddH2O
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
Synonyms N/A

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 (g) = Concentration (mol/L) × Volume (L) × 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

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

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