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Synonyms | APO866 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H29N3O2 |
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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. |
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. |
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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] |
細胞アッセイ | 細胞株 | 41 hematologic malignant cell lines |
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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. |
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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 |
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.]
Integration of 3D bioprinting and multi-algorithm machine learning identified glioma susceptibilities and microenvironment characteristics [ Cell Discov, 2024, 10(1):39] | PubMed: 38594259 |
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 |
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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