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| Targets |
NLG-1489 targets indoleamine 2,3-dioxygenase (IDO), an enzyme that catalyzes the rate-limiting step in the catabolism of tryptophan along the kynurenine pathway. IDO is a heme-containing enzyme that is induced by inflammatory cytokines such as IFN-gamma and plays a critical role in immune regulation. IDO-mediated tryptophan depletion and kynurenine production suppress T cell proliferation and promote immune tolerance, contributing to tumor immune escape. By inhibiting IDO with an IC50 of 1-10 microM, NLG-1489 restores tryptophan levels and reduces kynurenine production, thereby enhancing antitumor immune responses.
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| ln Vitro |
IDO-IN-5 (Compound 1487) is an inhibitor of indoleamine 2,3-dioxygenase (IDO) with an IC50 of 1–10 μM (the concentration at which recombinant IDO-IN inhibits 50% of enzyme activity) [1].
NLG-1489 demonstrates potent in vitro activity as an IDO inhibitor. The compound inhibits IDO with an IC50 of 1-10 microM. Its activity is concentration-dependent, with potent inhibition observed at appropriate concentrations. NLG-1489 has anticancer and immunomodulatory activity. The compound's ability to inhibit IDO activity has been characterized in enzymatic assays using recombinant IDO enzyme or cell-based assays measuring kynurenine production. NLG-1489 is extracted from patent WO WO2012142237A1, compound 1489. Its potency and selectivity for IDO make it a valuable tool for studying IDO biology and evaluating IDO inhibition as a therapeutic strategy for cancer immunotherapy. |
| ln Vivo |
In vivo, NLG-1489 has been studied for its potential to enhance antitumor immune responses. As an IDO inhibitor, the compound would be expected to restore tryptophan levels and reduce kynurenine production, thereby enhancing T cell proliferation and antitumor immunity. IDO inhibitors have been studied in various animal models of cancer, where they have demonstrated efficacy in enhancing antitumor immune responses and reducing tumor growth. NLG-1489's in vivo activity has been described in patent literature. The compound's immunomodulatory activity supports its potential for cancer immunotherapy research.
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| Enzyme Assay |
In vitro enzyme assays for NLG-1489 involve measuring the inhibition of IDO enzymatic activity. Recombinant human IDO is incubated with varying concentrations of the test compound, L-tryptophan, and appropriate cofactors (e.g., methylene blue, ascorbate, catalase). The production of kynurenine is quantified by measuring absorbance at 320 nm after deproteinization with trichloroacetic acid and reaction with Ehrlich's reagent. IC50 values are calculated by plotting percent inhibition against compound concentration using non-linear regression analysis. The compound has an IC50 of 1-10 microM. Each concentration is typically tested in duplicate or triplicate with appropriate positive controls (known IDO inhibitors) and vehicle controls.
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| Cell Assay |
In vitro cellular assays for NLG-1489 are performed using IDO-expressing cells, such as dendritic cells, macrophages, or cancer cells. Cells are stimulated with IFN-gamma to induce IDO expression and treated with varying concentrations of the compound. Kynurenine levels in the culture supernatant are measured by HPLC or by colorimetric assay after reaction with Ehrlich's reagent. Cell viability is assessed in parallel using standard viability assays such as MTT to ensure that observed effects are not due to cell death. The compound's ability to restore T cell proliferation in the presence of IDO-expressing cells can be assessed using T cell proliferation assays. IC50 values for inhibition of kynurenine production are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for NLG-1489 are conducted using mouse models of cancer. Immunocompetent mice are implanted with syngeneic tumor cells and treated with NLG-1489 via oral gavage or intraperitoneal injection at various doses and schedules. Tumor growth is measured using calipers. Immune cell infiltration into tumors is assessed by flow cytometry or immunohistochemistry. Tryptophan and kynurenine levels are measured in plasma and tumor tissues by LC-MS/MS. Cytokine levels are measured in serum and tumor tissues. Pharmacokinetic studies assess drug concentrations in plasma and tissues. Animals are monitored for clinical signs and body weight. Efficacy is expressed as tumor growth inhibition and immune activation compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NLG-1489 have been characterized in preclinical studies. The compound has a molecular formula of C18H21FN2O2 and a molecular weight of 316.37 g/mol. NLG-1489 is extracted from patent WO WO2012142237A1, compound 1489. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have been characterized in animal models. The compound's pharmacokinetic profile supports its use in preclinical studies of cancer immunotherapy. Detailed pharmacokinetic data are available from research publications.
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| Toxicity/Toxicokinetics |
NLG-1489 is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As an IDO inhibitor that modulates immune function, the compound would be expected to have effects on immune regulation and could potentially cause immune-related adverse events. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has been conducted as part of preclinical development. The compound is not approved for human use and is strictly intended for research purposes.
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| References | |
| Additional Infomation |
NLG-1489 (IDO-IN-5) is a novel and potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 1-10 microM. It is extracted from patent WO WO2012142237A1, compound 1489. NLG-1489 has anticancer and immunomodulatory activity. The compound has a molecular formula of C18H21FN2O2 and a molecular weight of 316.37 g/mol. NLG-1489 has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only.
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| Molecular Formula |
C₁₈H₂₁FN₂O₂
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|---|---|
| Molecular Weight |
316.37
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| Exact Mass |
316.158
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| CAS # |
1402837-79-9
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| Related CAS # |
IDO-IN-6;1402837-76-6;Navoximod;1402837-78-8;IDO-IN-8;1402837-77-7
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| PubChem CID |
70874201
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
555.4±35.0 °C at 760 mmHg
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| Flash Point |
289.7±25.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.683
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| LogP |
1.28
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
416
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1CC(CCC1[C@@H](C[C@@H]2C3=C(C=CC=C3F)C4=CN=CN24)O)O
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| InChi Key |
YGACXVRLDHEXKY-LRBMDJJVSA-N
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| InChi Code |
InChI=1S/C18H21FN2O2/c19-14-3-1-2-13-16-9-20-10-21(16)15(18(13)14)8-17(23)11-4-6-12(22)7-5-11/h1-3,9-12,15,17,22-23H,4-8H2/t11?,12?,15-,17-/m1/s1
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| Chemical Name |
4-[(1R)-2-[(5R)-6-fluoro-5H-imidazo[5,1-a]isoindol-5-yl]-1-hydroxyethyl]cyclohexan-1-ol
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| Synonyms |
NLG-1489NLG1489 (IDO-IN-5)
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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 | 3.1609 mL | 15.8043 mL | 31.6086 mL | |
| 5 mM | 0.6322 mL | 3.1609 mL | 6.3217 mL | |
| 10 mM | 0.3161 mL | 1.5804 mL | 3.1609 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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