受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C11H13BrFN7O4S |
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分子量 | 438.23 | CAS No. | 1204669-58-8 | ||||
Solubility (25°C)* | 体外 | DMSO | 88 mg/mL (200.8 mM) | ||||
Ethanol (warmed with 50ºC water bath) | 22 mg/mL (50.2 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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 | Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). |
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in vitro | In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. [1] |
in vivo | INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. [1] In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. [2] |
キナーゼアッセイ | IDO enzyme assays | |
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Human IDO with an N-terminal His tag is expressed in E.coli and purified to homogeneity. IDO catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays are performed at room temperature using 20 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 3.5 µM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates are recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine. | ||
細胞アッセイ | 細胞株 | Jurkat cells |
濃度 | 50 μM | |
反応時間 | 72 h | |
実験の流れ | Jurkat cells were incubated with serially diluted epacadostat for 72 h. Their viability was measured and analyzed as percentage of the non-treated control. |
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動物実験 | 動物モデル | Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors |
投薬量 | ~100 mg/kg, twice a day | |
投与方法 | p.o. |
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Data from [Data independently produced by , , FEBS J, 2016, doi: 10.1111/febs.13966.]
Data from [Data independently produced by , , Cancer Immunol Immunother, 2018, 67(8):1305-1315]
Data from [Data independently produced by , , Mol Immunol, 2018, 103:144-155]
Epacadostat stabilizes the apo-form of IDO1 and signals a pro-tumorigenic pathway in human ovarian cancer cells [ Front Immunol, 2024, 15:1346686] | PubMed: 38333210 |
Selective inhibition of indoleamine and tryptophan 2,3-dioxygenases: Comparative study on kynurenine pathway in cell lines via LC-MS/MS-based targeted metabolomics [ J Pharm Biomed Anal, 2024, 237:115750] | PubMed: 37804639 |
Targeting Tryptophan Catabolism in Ovarian Cancer to Attenuate Macrophage Infiltration and PD-L1 Expression [ Cancer Res Commun, 2024, 4(3):822-833] | PubMed: 38451784 |
An adverse tumor-protective effect of IDO1 inhibition [ Cell Rep Med, 2023, 4(2):100941] | PubMed: 36812891 |
A tryptophan metabolite prevents depletion of circulating endothelial progenitor cells in systemic low-grade inflammation [ Front Immunol, 2023, 14:964660] | PubMed: 37081894 |
The catalytic inhibitor epacadostat can affect the non-enzymatic function of IDO1 [ Front Immunol, 2023, 14:1134551] | PubMed: 37122718 |
Targeting the STAT5A/IDO1 axis overcomes radioresistance and reverses the immunosuppressive tumor microenvironment in NSCLC [ Int J Oncol, 2023, 62(1)12] | PubMed: 36453241 |
IDO1 Promotes the Progression of NSCLC by Regulating the Polarization of M2 Macrophages [ Int J Gen Med, 2023, 16:1713-1733] | PubMed: 37187591 |
Anakinra restores cellular proteostasis by coupling mitochondrial redox balance to autophagy [ J Clin Invest, 2022, 132(2)e144983] | PubMed: 34847078 |
IDO-1 inhibitor INCB24360 elicits distant metastasis of basal extruded cancer cells in pancreatic ductal adenocarcinoma [ Acta Pharmacol Sin, 2022, 10.1038/s41401-022-01035-w] | PubMed: 36517670 |
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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