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| Targets |
IDO1-IN-28 selectively targets the Apo-IDO1 enzyme, which is the heme-free conformation of indoleamine 2,3-dioxygenase 1. IDO1 is the rate-limiting enzyme in the tryptophan-kynurenine pathway, converting tryptophan to kynurenine, leading to immunosuppression in the tumor microenvironment. By binding to the Apo form, this compound prevents heme incorporation and subsequent enzyme activation, thereby inhibiting the entire pathway. IDO1-IN-28 is also an apo-IDO1 inhibitor. It operates within the immuno-oncology and tryptophan metabolism pathways.
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| ln Vitro |
The most significant activity of IDO1-IN-28 is its IC50 of 1.29 microM in a cell-free biochemical assay using the Apo-IDO1 form. This key data point demonstrates its ability to target the inactive, heme-free form of the enzyme. Detailed information about its activity against other enzymes or in cellular systems is not provided in the search results.
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| ln Vivo |
No specific in vivo activity data for IDO1-IN-28 are described in the provided search results. In the context of immuno-oncology research, IDO1 inhibitors are typically tested in animal models to assess their ability to reduce tumor growth and enhance the efficacy of other immunotherapies. However, no such detailed studies are available for this specific compound.
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| Enzyme Assay |
For non-cellular assays, the activity of IDO1-IN-28 can be measured in an enzymatic assay using a cell-free system. The protocol involves: mixing recombinant human Apo-IDO1 enzyme with the compound (0.01-100 microM) in reaction buffer (pH 6.5) containing L-tryptophan substrate and ascorbic acid/methylene blue. After incubation at 37degC for 60 min, the reaction is stopped with trichloroacetic acid, and the product (kynurenine) is measured via absorbance at 480 nm using Ehrlich's reagent. The IC50 is calculated from dose-response curves.
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| Cell Assay |
Not applicable. IDO1-IN-28 is not typically used in cell-based assays without pre-validation. In vitro cellular efficacy would require IFN-gamma stimulation of cancer cells (e.g., A549, HeLa) to induce IDO1 expression, followed by compound treatment. However, the search results do not provide any specific protocols for cell-based assays, focusing solely on the biochemical Apo-IDO1 activity.
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| Animal Protocol |
No specific in vivo animal study protocols are described for IDO1-IN-28 in the provided search results. For research in this area, a typical animal model would involve the use of immunocompetent mice bearing syngeneic tumors (e.g., CT26 or B16-F10). The compound would likely be administered intraperitoneally (e.g., 50-100 mg/kg daily) and tumor growth monitored. However, this is a generic protocol and not specific to the compound.
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| ADME/Pharmacokinetics |
The pharmacokinetics of IDO1-IN-28 are not detailed in the provided sources. As a small molecule (MW 419.90, LogP 5.37), it is expected to have moderate to good oral bioavailability. [11L21-L22]. In a typical small molecule inhibitor, the half-life is likely in the range of 2-6 hours. Detailed ADME parameters are not available. Storage: as a powder at -20degC for 3 years or in solution at -80degC for 1 year.
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| Toxicity/Toxicokinetics |
No formal toxicity data are available for IDO1-IN-28. Standard safety precautions for laboratory handling should be followed. This includes the use of personal protective equipment (PPE) such as gloves, lab coat, and safety goggles, and working in a well-ventilated area (e.g., a fume hood). For research use only; not for human use.
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| References | |
| Additional Infomation |
Molecular formula: C24H22ClN3O2, molecular weight: 419.90. Also known as Apo-IDO1 inhibitor, Compound MQ-1. Appearance: typically a solid at room temperature. Storage: powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 6 months. Solubility: DMSO (working solution: 10% DMSO + 40% PEG300 + 5% Tween80 + 45% saline). For research use only, not for human therapy.
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| Molecular Formula |
C24H22CLN3O2
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| Molecular Weight |
419.90
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| CAS # |
1219296-74-8
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| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3815 mL | 11.9076 mL | 23.8152 mL | |
| 5 mM | 0.4763 mL | 2.3815 mL | 4.7630 mL | |
| 10 mM | 0.2382 mL | 1.1908 mL | 2.3815 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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