Daporinad (FK866)

製品コードS2799 バッチS279904

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
* <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 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]
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]

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. 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.
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

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：

Decreased liver B vitamin-related enzymes as a metabolic hallmark of cancer cachexia [ Nat Commun, 2023, 14(1):6246] PubMed: 37803016
Decreased liver B vitamin-related enzymes as a metabolic hallmark of cancer cachexia [ Nat Commun, 2023, 14(1):6246] PubMed: 37803016
NAD+ Metabolism Generates a Metabolic Vulnerability in Endocrine-Resistant Metastatic Breast Tumors in Females [ Endocrinology, 2023, 164(6)bqad073] PubMed: 37170651
Improving lysosomal ferroptosis with NMN administration protects against heart failure [ Life Sci Alliance, 2023, 6(12)e202302116] PubMed: 37793777
Improving lysosomal ferroptosis with NMN administration protects against heart failure [ Life Sci Alliance, 2023, 6(12)e202302116] PubMed: 37793777
DePARylation is critical for S phase progression and cell survival [ bioRxiv, 2023, 2023.07.31.551317] PubMed: 37577639
DePARylation is critical for S phase progression and cell survival [ bioRxiv, 2023, 2023.07.31.551317] PubMed: 37577639
Discovery of small-molecule activators of nicotinamide phosphoribosyltransferase (NAMPT) and their preclinical neuroprotective activity [ Cell Res, 2022, 10.1038/s41422-022-00651-9] PubMed: 35459935
secDrug: a pipeline to discover novel drug combinations to kill drug-resistant multiple myeloma cells using a greedy set cover algorithm and single-cell multi-omics [ Blood Cancer J, 2022, 12(3):39] PubMed: 35264575
Regulation of reverse electron transfer at mitochondrial complex I by unconventional Notch action in cancer stem cells [ Dev Cell, 2022, 57(2):260-276.e9] PubMed: 35077680

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。