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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Cited by 5 Publications

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 NGPT[|dEgXSxdH;4bYPDqGG|c3H5 NFS0fndEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iC2b4ThcEBk\WyudXzhdkBPSURqUDmgcIV3\WxuIFnDOVA:OC53IH7N MWixPVk3OTF6Mx?=
human A2780 cells M1\ESHBzd2yrZnXyZZRqd25iYYPzZZk> NIjEdYU4OiCq MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGy|IHHmeIVzKDd{IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBKSzVyPUGgcm0> NIHYOlczPDRyNUSxPS=>
human NYH cells M2\aUGN6fG:2b4jpZ:Kh[XO|YYm= MnSyN{B4\WWtcx?= NXXYbnFbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVlmKIHPlcIx{KGGodHXyJFMhf2Wna4OgZpkh[2yxbn;n[Y5q[yC|dYL2bZZidCCjc4PhfUwhUUN3ME2xMlUhdk1? M3H0PVI{Pjd7OUG1
human HepG2 cells NVf0WXNvTnWwY4Tpc44h[XO|YYm= NFLi[nQyKGh? MoXVTY5pcWKrdHnvckBw\iCQQV3QWEBqdiCqdX3hckBJ\XCJMjDj[YxteyC3c3nu[{BcOTSFXT3ubYNwfGmwYX3p[IUwWFKSUDDhd{B{fWK|dILheIUh[XO|ZYPz[YQh[XNiZn;ycYF1cW:wIH;mJHsyPEOfLX7pZ491cW6jbXnk[UBud26xboXjcIVwfGmmZTDh[pRmeiBzIHjyJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6pIHHuZYx6e2m|LDDJR|UxRTJwMjDuUS=> MUCyOFE3PDB6Nh?=
human PC3 cells Ml\2R5l1d3SxeHnjxsBie3OjeR?= M4jZZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVMvQCCwTR?= MVGyOFE3PDB6Nh?=
human A431 cells NEXqfHFEgXSxdH;4bYPDqGG|c3H5 NH36OoZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVA:Pi5zIH7N MkfoNlQyPjRyOE[=
human K562 cells MXvDfZRwfG:6aXRCpIF{e2G7 MUG5OkBp M2XPOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME23MlIhdk1? MWWyN|Y4QTlzNR?=
human MCF-7 cells NGDxem1EgXSxdH;4bYPDqGG|c3H5 NUHrPW5zPzJiaB?= MULDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2YuPyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVA:Py52IH7N NUP6[Ix{OjRzNkSwPFY>
human HCT116 cells NEe1d5JEgXSxdH;4bYPDqGG|c3H5 M13I[|czKGh? NITTSFREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IGfTWE0yKGG|c3H5MEBKSzVyPUGwMlkhdk1? NUG0cGxUOjRzNkSwPFY>
human HT1080 cells NEHaTm1EgXSxdH;4bYPDqGG|c3H5 M3vx[lYh\GG7cx?= NIfMe|dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXDFyOECgZ4VtdHNiYX\0[ZIhPiCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjF4IN88US=> MoXmNlE{OzByMUW=
human HCT116 cells NUnLR41FS3m2b4TvfIlkyqCjc4PhfS=> M{DEW|Yh\GG7cx?= NF\jXGpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPiCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjF4IN88US=> MWKyNVM{ODBzNR?=
human A549 cells MWHDfZRwfG:6aXRCpIF{e2G7 NGHKeIg3KGSjeYO= NV\McmxkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOTZizszN MoHpNlE{OzByMUW=
human SNU638 cells MnLzR5l1d3SxeHnjxsBie3OjeR?= NFPjdFQ3KGSjeYO= M3vCeWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNPXTZ|ODDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOTZizszN NWnhS3VqOjF|M{CwNVU>
human SKOV3 cells MXrDfZRwfG:6aXRCpIF{e2G7 NGLld5pEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTJzMTDuUS=> NWGwOYFOOjRzNkSwPFY>
human MCF7 cells MYDGeY5kfGmxbjDhd5NigQ>? NFj5[JMyOCEQvF2= M17QXlYh\GG7cx?= Ml22RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDheEAyOCC3TTDh[pRmeiB4IHThfZMh[nliU2LCJIF{e2G7LDDJR|UxRTBwNkig{txO NFTCUo4zOTN|MECxOS=>

... 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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID