FK866 (Daporinad)

Catalog No.S2799 Batch:S279902

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Technical Data

Formula

C24H29N3O2
Molecular Weight 391.51 CAS No. 658084-64-1
Solubility (25°C)* In vitro DMSO 80 mg/mL (204.33 mM)
Ethanol 78 mg/mL (199.22 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description FK866 (Daporinad) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. This compound triggers autophagy. Phase 1/2.
Targets
NMPRTase [5]
(Cell-free assay)
0.4 nM(Ki)
In vitro FK866 (Daporinad) 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. At concentrations ranging from 0-10 nM, this compound induces cell death, an effect independent of caspase activation but associated with depolarization of mitochondrial membrane. It also dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells at concentrations ranging from 0-10 nM. [1] At a concentration of 10 nM, it inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells. [2]
In vivo FK866 (Daporinad) administered intraperitoneally at a dose of 20 mg/kg twice a day for 4 days, repeated weekly over 3 weeks, prevents and abrogates tumor growth in C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. [1] At a dose of 0.12 mg/kg/hour, this compound prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA. [2]

Protocol (from reference)

Cell Assay:

[1]
  • 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. FK866 (Daporinad) 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 this compound 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.
Animal Study:

[1]
  • 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

References

  • https://pubmed.ncbi.nlm.nih.gov/19196867/
  • https://pubmed.ncbi.nlm.nih.gov/21400478/
  • https://pubmed.ncbi.nlm.nih.gov/20515945/
  • https://pubmed.ncbi.nlm.nih.gov/20696207/
  • https://pubmed.ncbi.nlm.nih.gov/14612543/

Customer Product Validation

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.

Data from [ Mol Endocrinol , 2014 , 28(3), 395-405 ]

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.

Data from [ , , Drug Des Devel Ther, 2015, 9: 1511-54 ]

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).

Data from [ , , Cancer Lett, 2016, 379(1):1-11. ]

Immunofluorescence analysis of Aggrecan and Collagen II expression in NP cells.

Data from [ , , Cell Physiol Biochem, 2018, 49(6):2463-2482 ]

Selleck's FK866 (Daporinad) Has Been Cited by 79 Publications

ROS-Responsive Hydrogel for Localized Delivery of Nampt and Stat3 Inhibitors Exhibits Synergistic Antitumor Effects in Colorectal Cancer Through Ferroptosis Induction and Immune Microenvironment Remodeling [ Adv Sci (Weinh), 2025, 12(33):e06599] PubMed: 40492508
Targeting SARM1 as a novel neuroprotective therapy in neurotropic viral infections [ J Neuroinflammation, 2025, 22(1):113] PubMed: 40254576
NAMPT and NNMT released via extracellular vesicles and as soluble mediators are distinguished traits of BRAF inhibitor resistance of melanoma cells impacting on the tumor microenvironment [ Cell Commun Signal, 2025, 23(1):348] PubMed: 40691620
SIRT5-mediated desuccinylation of the porcine deltacoronavirus M protein drives pexophagy to enhance viral proliferation [ PLoS Pathog, 2025, 21(5):e1013163] PubMed: 40344161
Inhibition of TRAF3IP2 Modulates NAMPT and NAD Metabolism in Glioblastoma [ J Neuroimmune Pharmacol, 2025, 20(1):95] PubMed: 41123804
Dual Roles of Canagliflozin on Cholangiocarcinoma Cell Growth and Enhanced Growth Suppression in Combination with FK866 [ Int J Mol Sci, 2025, 26(3)978] PubMed: 39940750
Efficacy of NAMPT inhibition in T-cell acute lymphoblastic leukemia [ PLoS One, 2025, 20(6):e0324443] PubMed: 40526635
PARP1 promotes replication-independent DNA double-strand break formation after acute DNA-methylation damage [ bioRxiv, 2025, 2025.07.10.663928] PubMed: 40672314
NAPRT expression and epigenetic regulation in pediatric rhabdomyosarcoma as a potential biomarker for NAMPT inhibition [ bioRxiv, 2025, 2025.07.28.667284] PubMed: 40766550
Integration of 3D bioprinting and multi-algorithm machine learning identified glioma susceptibilities and microenvironment characteristics [ Cell Discov, 2024, 10(1):39] PubMed: 38594259

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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