IDO-IN-1
(Synonyms: 4-氨基-N-(3-溴-4-氟苯基)-N'-羟基-1,2,5-恶二唑-3-甲脒) 目录号 : GC15876
A potent IDO inhibitor
Cas No.:914638-30-5
Sample solution is provided at 25 µL, 10mM.
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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:
[1] Yue EW, et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J Med Chem. 2009 Dec 10;52(23):7364-7.
| Cas No. | 914638-30-5 | SDF | |
| 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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1636 mL | 15.8178 mL | 31.6356 mL |
| 5 mM | 0.6327 mL | 3.1636 mL | 6.3271 mL |
| 10 mM | 0.3164 mL | 1.5818 mL | 3.1636 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet