Home Metabolism Transferase inhibitor - NAMPT inhibitor - Autophagy activator Daporinad (FK866) For research use only.

Daporinad (FK866)

Synonyms: APO866

Daporinad (FK866) 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.

Daporinad (FK866) Chemical Structure

Daporinad (FK866) Chemical Structure

CAS No. 658084-64-1

Purity & Quality Control

Products often used together with Daporinad (FK866)

KPT 9274 (ATG-019)

Daporinad and KPT 9274 are NMPT inhibitors and can strongly decrease total NAD+ levels and mitochondrial respiration in M2 macrophages.

Weinhauser I, et al. Sci Adv. 2023 Apr 14;9(15):eadf8522.

GMX1778

Daporinad and GMX1778 are iNAMPT enzymatic inhibitors that have been developed as anti-cancer treatment options.

Sun BL, et al. EBioMedicine. 2020 Nov;61:103059.

Daporinad (FK866) Related Products

Signaling Pathway

Transferase Signaling Pathways

Transferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SH-SY5Y Cytotoxicity assay Cytotoxicity against human SH-SY5Y cells assessed as reduction of total cellular NAD(P) level, IC50 = 0.0005 μM. 19961183
SH-SY5Y Cytotoxicity assay 48 hrs Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0017 μM. 19961183
HT1080 Cytotoxicity assay 6 days Cytotoxicity against human HT1080 cells after 6 days by SRB assay, IC50 = 0.16 μM. 21330015
A549 Cytotoxicity assay 6 days Cytotoxicity against human A549 cells after 6 days by SRB assay, IC50 = 0.16 μM. 21330015
HCT116 Cytotoxicity assay 6 days Cytotoxicity against human HCT116 cells after 6 days by SRB assay, IC50 = 0.16 μM. 21330015
SNU638 Cytotoxicity assay 6 days Cytotoxicity against human SNU638 cells after 6 days by SRB assay, IC50 = 0.16 μM. 21330015
MCF7 Antitumor assay 10 uM 6 days Antitumor activity against human MCF7 cells at 10 uM after 6 days by SRB assay, IC50 = 0.68 μM. 21330015
K562 Cytotoxicity assay 6 days Cytotoxicity against human K562 cells after 6 days by SRB assay, IC50 = 20 μM. 21330015
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells after 72 hrs by SRB assay, IC50 = 0.001 μM. 23617784
NYH Cytotoxicity assay 3 weeks Cytotoxicity against human NYH cells after 3 weeks by clonogenic survival assay, LD50 = 0.0015 μM. 23679915
K562 Cytotoxicity assay 96 hrs Cytotoxicity against human K562 cells after 96 hrs by MTT assay, IC50 = 0.0072 μM. 23679915
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis, IC50 = 0.001 μM. 23859118
NYH Cytotoxicity assay Cytotoxicity against human NYH cells by clonogenic assay, IC50 = 0.0015 μM. 24164086
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0016 μM. 24164086
HepG2 Function assay 1 hr Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis, IC50 = 0.0022 μM. 24164086
PC3 Cytotoxicity assay Cytotoxicity against human PC3 cells by clonogenic assay, IC50 = 0.0038 μM. 24164086
A2780 Cytotoxicity assay Cytotoxicity against human A2780 cells by clonogenic assay, IC50 = 0.0057 μM. 24164086
A431 Cytotoxicity assay Cytotoxicity against human A431 cells by clonogenic assay, IC50 = 0.0061 μM. 24164086
MCF-7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0074 μM. 24164086
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by clonogenic assay, IC50 = 0.0084 μM. 24164086
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0109 μM. 24164086
SKOV3 Cytotoxicity assay Cytotoxicity against human SKOV3 cells by clonogenic assay, IC50 = 0.211 μM. 24164086
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against APO866-resistant human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.946 μM. 24164086
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay, IC50 = 0.001 μM. 24405419
A2780 Function assay 72 hrs Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay, IC50 = 0.001 μM. 27541271
DE3 Function assay 15 mins Inhibition of human full length C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta (DE3) cells using nicotinamide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins in presence of PRPP, IC50 = 0.003 μM. 27541271
SH-SY5Y Cytotoxicity assay 56 hrs Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 56 hrs by MTT assay, EC50 = 0.0034 μM. 28165742
A2780 Cytotoxicity assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability, IC50 = 0.0042 μM. 28165742
PC3 Antiproliferative assay 5 days Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay, IC50 = 0.0057 μM. 28610984
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 0.89 μM. 28885834
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.3 μM. 28885834
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.6 μM. 28885834
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.89 μM. 29348808
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.6 μM. 29348808
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 3.7 μM. 29348808
SH-SY5Y Autophagy assay 40 hrs Induction of autophagy in human SH-SY5Y cells assessed as LC3/phosphotidylethanolamine coupling after 40 hrs by Western blot analysis 19961183
MCF7 Antitumor assay 6 days Antitumor activity against human MCF7 cells after 6 days by SRB assay 21330015
MDCK Function assay 10 uM Apparent permeability across apical to basolateral side in dog MDCK cells at 10 uM by LC-MS/MS analysis 23859118
DU145 Cytotoxicity assay Cytotoxicity against human DU145 cells by clonogenic assay 24164086
MCF7 Cytotoxicity assay 96 hrs Cytotoxicity against human MCF7 cells after 96 hrs by clonogenic assay 24164086
HCT116 Function assay Resistance factor, ratio of IC50 for APO866-resistant human HCT116 cells to IC50 for human HCT116 cells 24164086
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay in presence of nicotinamide mononucleotide 24405419
Sf9 Function assay 30 mins Inhibition of recombinant full length human C-terminal His/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay 29348808
Click to View More Cell Line Experimental Data

Biological Activity

Description Daporinad (FK866) 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.
Targets
NMPRTase [5]
(Cell-free assay)
0.4 nM(Ki)
In vitro
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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot SIRT1 p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1 AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448) 29905535
Immunofluorescence pMLKL phGSK3β ph-β-catenin 29996103
Growth inhibition assay Cell viability 27462772
In Vivo
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]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00435084 Completed
B-cell Chronic Lymphocytic Leukemia
Valerio Therapeutics
 February 2007 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 391.51 Formula

C24H29N3O2
CAS No. 658084-64-1 SDF Download Daporinad (FK866) SDF
Smiles C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (199.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 78 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

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.

Tags: buy Daporinad (FK866) | Daporinad (FK866) supplier | purchase Daporinad (FK866) | Daporinad (FK866) cost | Daporinad (FK866) manufacturer | order Daporinad (FK866) | Daporinad (FK866) distributor