| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
| Targets |
IDO
The primary target of (Rac)-Indoximod is indoleamine 2,3-dioxygenase (IDO), an enzyme involved in tryptophan metabolism. By inhibiting IDO, (Rac)-Indoximod prevents tryptophan depletion and the accumulation of immunosuppressive kynurenines, thereby restoring T cell proliferation and function. Co-treatment with IFN-γ and (Rac)-Indoximod markedly reduces the activity of human cardiac myofibroblasts expressing α-SMA and induces apoptosis through up-regulating the IRF-1, Fas, and FasL genes. |
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| ln Vitro |
(Rac)-Indoximod (1-methyl-DL-tryptophan; 0.5 mM; 3 days) prevents tryptophan depletion independent of tryptophan depletion, but it also inhibits tryptophan elimination, partially reversing the growth inhibitory action of IFN-γ. may cause cellular death [1].
In vitro, (Rac)-Indoximod (0.5 mM; 3 days) inhibits tryptophan depletion, thereby partially reversing the growth-inhibitory activity of IFN-γ. However, it eventually induces cell death regardless of tryptophan depletion. Co-treatment with IFN-γ and (Rac)-Indoximod markedly reduces the activity of human cardiac myofibroblasts (hCMs) expressing α-SMA and induces apoptosis through up-regulating the IRF-1, Fas, and FasL genes. The compound is a potent IDO inhibitor used in cancer immunotherapy research. |
| ln Vivo |
In vivo activity of (Rac)-Indoximod has been studied in cancer immunotherapy models. As an IDO pathway inhibitor, it is used to overcome tumor-induced immune suppression and enhance anti-tumor immune responses. The compound is the racemic form of Indoximod and has been investigated in preclinical and clinical studies for the treatment of various cancers. It is often used in combination with other immunotherapies, such as checkpoint inhibitors, to improve therapeutic outcomes.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for (Rac)-Indoximod typically involve IDO enzyme inhibition studies. The enzyme is incubated with varying concentrations of (Rac)-Indoximod (0.1-1000 µM) in appropriate buffer at 37°C. IDO activity is measured by monitoring the conversion of tryptophan to kynurenine using spectrophotometric or HPLC methods. The IC₅₀ value is calculated from the dose-response curve. The compound demonstrates concentration-dependent inhibition of IDO activity.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Human cardiac myofibroblasts (hCMs) Tested Concentrations: 0.5 mM Incubation Duration: 3 days Experimental Results: Growth retardation by IFN-γ was partially reversed on day 2, but cell viability was further decreased on day 3. In vitro cellular assays for (Rac)-Indoximod involve testing its effects on IDO activity and immune cell function. Cells are treated with varying concentrations of (Rac)-Indoximod (0.01-10 mM) for 24-72 hours. Tryptophan depletion and kynurenine production are measured by HPLC or mass spectrometry. T cell proliferation and function are assessed by flow cytometry or ELISA. The compound demonstrates concentration-dependent inhibition of IDO activity and restoration of T cell function. |
| Animal Protocol |
In vivo animal studies for (Rac)-Indoximod involve efficacy testing in tumor-bearing models. Mice implanted with cancer cells are treated with (Rac)-Indoximod via oral administration at various doses. Tumor volume and body weight are monitored over 2-4 weeks. Immune cell infiltration and activation in tumors are assessed by flow cytometry or immunohistochemistry. The compound demonstrates anti-tumor activity and immunomodulatory effects in vivo when used alone or in combination with other immunotherapies.
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| ADME/Pharmacokinetics |
(Rac)-Indoximod has a molecular formula of C₁₂H₁₄N₂O₂ and a molecular weight of 218.25. It appears as a solid with a purity of ≥98%. It is soluble in water at 2.5 mg/mL. The compound is intended for research use only and is not approved for clinical use. (Rac)-Indoximod is used in cancer immunotherapy research as an IDO pathway inhibitor.
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| Toxicity/Toxicokinetics |
The toxicity profile of (Rac)-Indoximod has been characterized in preclinical studies. As an IDO inhibitor, it is generally well-tolerated. Standard toxicity studies include assessment of body weight changes, hematological parameters, and histopathological examination of major organs in animal models. The compound is intended for research use only and is not approved for clinical use.
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| References | |
| Additional Infomation |
1-Methyltryptophan is a tryptophan derivative with a methyl substituent at the 1-position of its indole ring. It is an EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor and an antitumor drug. It is a non-protein α-amino acid and a derivative of tryptophan. 1-Methyl-DL-tryptophan has been reported to exist in Aspergillus fumigatus, and relevant data are available. See also: 1-Methyl-L-tryptophan (note moved here).
(Rac)-Indoximod (CAS 26988-72-7) is a racemic IDO inhibitor, also known as 1-Methyl-DL-tryptophan or (Rac)-NLG-8189. It has a molecular formula of C₁₂H₁₄N₂O₂ and a molecular weight of 218.25. The compound inhibits IDO, preventing tryptophan depletion and restoring T cell function. It is used in cancer immunotherapy research. (Rac)-Indoximod is intended for research use only and is not approved for clinical use. |
| Molecular Formula |
C12H14N2O2
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|---|---|
| Molecular Weight |
218.251762866974
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| Exact Mass |
218.106
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| CAS # |
26988-72-7
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| Related CAS # |
Indoximod;110117-83-4;(S)-Indoximod;21339-55-9
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| PubChem CID |
98112
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| Appearance |
White to off-white solid powder
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| Density |
1.28g/cm3
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| Boiling Point |
429.3ºC at 760mmHg
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| Melting Point |
250ºC (dec.)(lit.)
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| Flash Point |
213.4ºC
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| LogP |
1.833
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
270
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(C(CC1=CN(C)C2C=CC=CC1=2)N)=O
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| InChi Key |
ZADWXFSZEAPBJS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H14N2O2/c1-14-7-8(6-10(13)12(15)16)9-4-2-3-5-11(9)14/h2-5,7,10H,6,13H2,1H3,(H,15,16)
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| Chemical Name |
2-amino-3-(1-methylindol-3-yl)propanoic acid
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
0.1 M NaOH : 10 mg/mL (45.82 mM)
DMSO : 4.76 mg/mL (21.81 mM) |
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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 | 4.5819 mL | 22.9095 mL | 45.8190 mL | |
| 5 mM | 0.9164 mL | 4.5819 mL | 9.1638 mL | |
| 10 mM | 0.4582 mL | 2.2910 mL | 4.5819 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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