| CAS NO: | 914638-30-5 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 914638-30-5 |
| 别名 | 4-氨基-N-(3-溴-4-氟苯基)-N'-羟基-1,2,5-恶二唑-3-甲脒 |
| 化学名 | 4-amino-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide |
| Canonical SMILES | FC1=CC=C(/N=C(C2=NON=C2N)\NO)C=C1Br |
| 分子式 | C9H7BrFN5O2 |
| 分子量 | 316.1 |
| 溶解度 | ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 59 nM IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor. IDO is expressed in various tissues throughout the body but mainly in cells within the immune system where it is induced in dendritic cells and macrophages at sites of inflammation by cytokines. The overexpression of IDO has been implicated in a variety of diseases, such as cancer, neurodegenerative disorders, age-related cataract, and HIV encephalitis. In vitro: In previous study, IDO-IN-1 was found to have improved in-vitro human intrinsic clearances without loss in IDO cellular potency [1]. In vivo: IDO-IN-1 analog, named 5l, was chosen for further in vivo studies because of its improved physical chemical properties compared to IDO-IN-1. The efficacy of 5l was tested in C57BL/6 mice with GMCSF-secreting B16 tumors, where 1-MT had previously shown activity. Results showed that the dose-dependent inhibition of tumor growth was linked to increasing exposures of 5l in plasma. In addition, a maximal effect of 50% tumor growth control (TGC) was observed when 5l was subcutaneously administered at 75 mg/kg bid. For comparison, 1-MT showed around 45% TGC when administered as subcutaneous pellets [1]. Clinical trial: Up to now, IDO-IN-1 is still in the preclinical development stage. Reference: |
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