| 货号 | 18265-1mg |
| 描述 | Indoleamine 2,3-dioxygenase (IDO) metabolizes tryptophan to kynurenine, leading to the production of NAD+via the kynurenine pathway. It has been implicated in mediating pathological immunosuppression associated with certain diseases, including cancer. INCB024360 analog is a potent IDO1 inhibitor that demonstrates IC50 values of 67 and 19 nM for human IDO in enzymatic activity and HeLa cell assays, respectively.1,2,3 It is inactive against tryptophan 2,3-dioxygenase (IC50 > 10 µM).2 At 25-75 mg/kg, subcutaneous administration of INCB024360 analog to mice significantly decreased kynurenine levels in plasma and dose-dependently reduced the growth of GM-CSF-secreting B16 tumor xenografts.2 A fluorine-18 moiety has been used to label this compound for use as a probe for imaging IDO1 expression via positron emission tomography.4 |
| 别名 | IDO5L; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Liu, X.,Shin, N.,Koblish, H.K., et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood 115(17), 3520-3530 (2010). 2.Yue, E.W.,Douty, B.,Wayland, B., et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. Journal of Medicinal Chemistry 52(23), 7364-7367 (2009). 3.Tomek, P.,Palmer, B.D.,Flanagan, J.U., et al. Formation of an N-formylkynurenine-derived fluorophore and its use for measuring indoleamine 2,3-dioxygenase 1 activity. Analytical and Bioanalytical Chemistry 405(8), 2515-2524 (2013). 4.Huang, X.,Gillies, R.J., and Tian, H. Synthesis of [18 F] 4-amino-N-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): A novel potential PET probe for imaging of IDO1 expression. Journal of Labelled Compounds and Radiopharmaceuticals 58(4), 156-162 (2015). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 271.6 |
| 分子式 | C9H7ClFN5O2 |
| CAS号 | 914471-09-3 |
| 稳定性 | ≥ 2 years |
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