IDO-IN-1 |
| Katalog-Nr.GC15876 |
IDO-IN-1 ist ein potenter Indolamin-2,3-Dioxygenase (IDO)-Hemmer mit einem IC50 von 59 nM.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | 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 | ||
| Formula | C9H7BrFN5O2 | M.Wt | 316.1 |
| Löslichkeit | ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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