受注:045-509-1970 |
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Synonyms | INCB14943 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C9H7ClFN5O2 |
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分子量 | 271.64 | CAS No. | 914471-09-3 | |
Solubility (25°C)* | 体外 | DMSO | 54 mg/mL warmed with 50ºC water bath (198.79 mM) | |
Ethanol | 54 mg/mL warmed with 50ºC water bath (198.79 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 | Epacadostat (INCB024360) analogue (INCB14943) is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM. Phase 2. |
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in vitro | In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 nM. [1] In coculture systems of human allogeneic lymphocytes with dendritic cells or tumor cells, INCB024360, via IDO1 inhibition, reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs, and increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells. [2] |
in vivo | In mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. [1] INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice. [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. | ||
動物実験 | 動物モデル | Mice bearing GM-CSF-secreting B16 tumors |
投薬量 | 75 mg/kg b.i.d | |
投与方法 | s.c. |
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Granulocytic myeloid-derived suppressor cells increase infection risk via the IDO/IL-10 pathway in patients with hepatitis B virus-related liver failure [ Front Immunol, 2022, 13:966514] | PubMed: 36685516 |
[ Oncoimmunology, 2017, ] | PubMed: 29209565 |
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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