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Indoximod (NLG-8189) 是一种具有口服具有活力的吲哚胺2,3-双加氧酶(IDO) 途径抑制剂。它在调节 mTOR 中充当 Trp 模拟物。它是一种可用于癌症研究的免疫代谢佐剂。
Indoximod (NLG-8189) 是一种具有口服具有活力的吲哚胺2,3-双加氧酶(IDO) 途径抑制剂。它在调节 mTOR 中充当 Trp 模拟物。它是一种可用于癌症研究的免疫代谢佐剂。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50 mg | ¥ 128 | 现货 | |
100 mg | ¥ 153 | 现货 | |
500 mg | ¥ 463 | 现货 | |
1 g | ¥ 637 | 现货 |
产品描述 | Indoximod (NLG-8189) is a methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2, 3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy. |
靶点活性 | IDO:19 μM(Ki) |
体外活性 | Indoximod significantly reverses the suppression of T cells created by IDO-expressing dendritic cells, using both human monocyte-derived dendritic cells and murine dendritic cells isolated directly from tumor-draining lymph nodes. [1] Indoximod activates a Trp sufficiency signal that stimulates mTOR, and relieves IDO-induced Trp deprivation as well as an autophagic response. [2] |
体内活性 | In mouse models of transplantable melanoma and transplantable and autochthonous breast cancer, Indoximod (400 mg/kg p.o.) enhances antitumor immunity in the setting of combined chemo-immunotherapy regimens. [1] |
激酶实验 | 1MT enantiomers are solubilized in DMSO containing 0.1N HCl and added at concentrations of 100, 50, and 0 μM to wells containing the reaction mixture with tryptophan (0-200 μM) followed by addition of IDO enzyme. Plates are sealed and incubated 1 hr in a humidified 37°C incubator, after which the reactions are terminated by addition of 12.5 μl 30% TCA per well. Plates are then resealed in plastic wrap, incubated 30 min at 50°C to hydrolyze the reaction product N-formylkynurenine to kynurenine, and centrifuged. Supernatants are transferred to a flat-bottom 96-well plate, mixed with 100 μl Ehrlich reagent and incubated 10 min at room temperature. Absorbance at 490 nm is read[1]. |
别名 | 吲哚莫德, NLG-8189, Indoximod (NLG-8189), 1-Methyl-D-tryptophan |
分子量 | 218.25 |
分子式 | C12H14N2O2 |
CAS No. | 110117-83-4 |
Smiles | Cn1cc(C[C@@H](N)C(O)=O)c2ccccc12 |
密度 | 1.28 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: Slightly soluble |
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