FK866 (Daporinad)

製品コードS2799 バッチS279903

印刷

化学情報

Chemical Structure Synonyms APO866 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H29N3O2
分子量 391.51 CAS No. 658084-64-1
Solubility (25°C)* 体外 DMSO 78 mg/mL (199.22 mM)
Ethanol 78 mg/mL (199.22 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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. It 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. This compound 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] It at concentration of 10 nM 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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 41 hematologic malignant cell lines
濃度 0 - 10 nM
反応時間 72 hours or 96 hours
実験の流れ

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.
動物実験 動物モデル C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
投薬量 20 mg/kg
投与方法 administered intraperitoneally twice a day for 4 days, repeated weekly over 3 weeks

参考

  • 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/

カスタマーフィードバック

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

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

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
Nicotinamide phosphoribosyltransferase prompts bleomycin-induced pulmonary fibrosis by driving macrophage M2 polarization in mice [ Theranostics, 2024, 14(7):2794-2815] PubMed: 38773984

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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