Navoximod
Based on 13 publication(s) in Google Scholar
Navoximod (GDC-0919; NLG-?919) is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.99%
- CAS 番号: 1402837-78-8
- 分子式: C18H21FN2O2
- 分子量:316.37
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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MedChemExpress（MCE）の使用を引用している文献 Navoximod
More- Nat Commun. 2022 Jul 12;13(1):4032. [Abstract]
- Adv Sci (Weinh). 2024 Dec 24:e2409790. [Abstract]
- Adv Sci (Weinh). 2023 Dec;10(35):e2305150. [Abstract]
- Adv Sci (Weinh). 2019 Apr 18;6(12):1900327. [Abstract]
- Chem Eng J. 478, 15 December 2023, 147465
- Nano Today. October 2022, 101600.
- J Immunother Cancer. 2025 May 30;13(5):e011398. [Abstract]
- Mater Today Bio. 2025 Jun 6:33:101954. [Abstract]
- J Cachexia Sarcopenia Muscle. 2023 Apr;14(2):1046-1059. [Abstract]
- ACS Appl Mater Interfaces. 2024 Jun 19;16(24):30671-30684. [Abstract]
- Cell Chem Biol. 2023 Aug 17;30(8):987-998.e24. [Abstract]
- Bioeng Transl Med. 2023 Oct 28;9(1):e10599. [Abstract]
- Toxicol Appl Pharmacol. 2017 May 15:323:74-80. [Abstract]
Customer Validation & Images
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WB
生物活性
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IDO 7 nM (Ki) |
IDO 75 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
434 nM
Compound: NLG-919
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Inhibition of IDO in human HeLa cells using tryptophan as substrate measured after 48 hrs in presence of INF gamma microplate reader analysis
Inhibition of IDO in human HeLa cells using tryptophan as substrate measured after 48 hrs in presence of INF gamma microplate reader analysis
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[PMID: 31223453] |
Using IDO-expressing human monocyte-derived dendritic cells (DCs) in allogeneic mixed lymphocyte reaction (MLR) reactions, Navoximod (NLG919) potently blocks IDO-induced T cell suppression and restores robust T cell responses with an ED50=80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, Navoximod abrogates IDO-induced suppression of antigen-specific T cells (OT-I) in vitro, with ED50=120 nM[1]. Navoximod inhibits the IDO activity in a concentration-dependent manner with an EC50 of 0.95?μM. PEG2k-Fmoc-NLG(L) is less active (EC50 of 3.4?μM) in inhibiting IDO compared with free Navoximod while PEG2k-Fmoc-NLG(S) is least active (EC50>10?μM). Coculture of IDO+tumor cells with splenocytes isolated from BALB/c mice leads to significant inhibition of T-cell proliferation. This inhibition is significantly attenuated when the mixed cells are treated with Navoximod. PEG2k-Fmoc-NLG(L) is also active in reversing the inhibitory effect of tumour cells although slightly less potent than Navoximod [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1402837-78-8
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性状 Solid
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分子量 316.37
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分子式 C18H21FN2O2
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Color White to light yellow
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SMILES
O[C@H](CC1)CC[C@]1([H])[C@H](O)C[C@@H]2N3C(C4=C2C(F)=CC=C4)=CN=C3
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別名
GDC-0919; NLG-919
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
Precision cancer sono-immunotherapy using deep-tissue activatable semiconducting polymer immunomodulatory nanoparticles. [Abstract]2022 Jul 12;13(1):4032. PMID: 35821238 -
Adv Sci (Weinh)
Pyruvate Kinase M2-Responsive Release of Paclitaxel and Indoleamine 2,3-Dioxygenase Inhibitor for Immuno-Chemotherapy of Nonsmall Cell Lung Cancer. [Abstract]2024 Dec 24:e2409790. PMID: 39716923 -
Adv Sci (Weinh)
Sono-Activatable Semiconducting Polymer Nanoreshapers Multiply Remodel Tumor Microenvironment for Potent Immunotherapy of Orthotopic Pancreatic Cancer. [Abstract]2023 Dec;10(35):e2305150. PMID: 37870196 -
Adv Sci (Weinh)
PI3Kgamma Inhibitor Attenuates Immunosuppressive Effect of Poly(l-Glutamic Acid)-Combretastatin A4 Conjugate in Metastatic Breast Cancer. [Abstract]2019 Apr 18;6(12):1900327. PMID: 31380170 -
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J Immunother Cancer
Neovascular pruning by IDO1 inhibitors can potentiate immunogenic cytotoxicity of ischemia-targeted agents to synergistically enhance anti-PD-1 responsiveness. [Abstract]2025 May 30;13(5):e011398. PMID: 40447318 -
Mater Today Bio
Extracellular matrix-degradable polymer nanostimulants elicit potent immune responses in orthotopic pancreatic cancer via sono-activatable dual-drug synergism. [Abstract]2025 Jun 6:33:101954. PMID: 40538751 -
J Cachexia Sarcopenia Muscle
Interleukin-6 promotes skeletal muscle catabolism by activating tryptophan-indoleamine 2,3-dioxygenase 1-kynurenine pathway during intra-abdominal sepsis. [Abstract]2023 Apr;14(2):1046-1059. PMID: 36880228
Navoximod purchased from MedChemExpress. Usage Cited in: J Cachexia Sarcopenia Muscle. 2023 Apr;14(2):1046-1059. [Abstract]
Navoximod reverses the decrease in MyHC level induced by CLP or LPS in GAS muscle, and increases the relative p-AKT/AKT level, in mice.
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ACS Appl Mater Interfaces
Reprogrammed IDO-Induced Immunosuppressive Microenvironment Synergizes with Immunogenic Magnetothermodynamics for Improved Cancer Therapy. [Abstract]2024 Jun 19;16(24):30671-30684. PMID: 38843203 -
Cell Chem Biol
2023 Aug 17;30(8):987-998.e24. PMID: 37490918 -
Bioeng Transl Med
Hydrophobic ion pairing and microfluidic nanoprecipitation enable efficient nanoformulation of a small molecule indolamine 2, 3-dioxygenase inhibitor immunotherapeutic. [Abstract]2023 Oct 28;9(1):e10599. PMID: 38193128 -
Toxicol Appl Pharmacol
2017 May 15:323:74-80. PMID: 28336214
溶剤 & 溶解度
DMSO : 100 mg/mL (316.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (9.48 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (9.48 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.58 mM); Clear solution
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
The IDO inhibitory effect of PEG2k-Fmoc-NLG is tested by an in vitro IDO assay. Briefly, HeLa cells are seeded in a 96-well plate at a cell density of 5000 cells per well and allowed to grow overnight. Recombinant human IFN-γ is then added to each well with a final concentration of 50 ng/mL. At the same time, various concentrations of PEG2k-Fmoc-NLG(L), PEG2k-Fmoc-NLG(S) or Navoximod (NLG919) (50 nM-20 μM) are added to the cells. After 48 h of incubation, 150 μL of the supernatants per well is transferred to a new 96-well plate. Seventy-five μL of 30% trichloroacetic acid is added into each well and the mixture is incubated at 50°C for 30 min to hydrolyse N-formylkynurenine to kynurenine. For colorimetric assay, supernatants are transferred to a new 96-well plate, mixed with equal volume of Ehrlich reagent (2% p-dimethylamino-benzaldehyde w/v in glacial acetic acid), and incubated for 10 min at RT. Reaction product is measured at 490 nm by a plate reader[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Mice are immobilized in a stereotactic frame for tumor implantation. Briefly, the skull is shaved and exposed with a 0.5 cm skin incision. With antiseptic technique, 105 GL261 cells (suspended in 3 μL RPMI-1640) are injected at the following coordinates with respect to the bregma on the right side (antero-posterior, -2 mm; medio-lateral, 2 mm; dorso-ventral, 3 mm). This placement reproducibly yielded tumor growth in a paracortical area of the posterolateral right frontal lobe. Tumor-bearing mice are treated with combinations of oral DL-1MT (2 mg/mL D-1MT mixed with 2 mg/mL L-1MT) in drinking water, D-1MT (4 mg/mL) in drinking water, Navoximod (6 mg/mL) in drinking water, intraperitoneal NSC-26271, intraperitoneal NSC 362856, and/or total-body radiation (500 cGy from a 137Cs source), as detailed in figure legends. Mice are observed daily, and sacrificed when they became ill or moribund[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (283 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Li M, et al. The indoleamine 2,3-dioxygenase pathway controls complement-dependent enhancement of chemo-radiation therapy against murine glioblastoma. J Immunother Cancer. 2014 Jul 7;2:21. [Content Brief]
[3]. Chen Y, et al. An immunostimulatory dual-functional nanocarrier that improves cancer immunochemotherapy. Nat Commun. 2016 Nov 7;7:13443. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1609 mL | 15.8043 mL | 31.6086 mL | 79.0214 mL |
| 5 mM | 0.6322 mL | 3.1609 mL | 6.3217 mL | 15.8043 mL | |
| 10 mM | 0.3161 mL | 1.5804 mL | 3.1609 mL | 7.9021 mL | |
| 15 mM | 0.2107 mL | 1.0536 mL | 2.1072 mL | 5.2681 mL | |
| 20 mM | 0.1580 mL | 0.7902 mL | 1.5804 mL | 3.9511 mL | |
| 25 mM | 0.1264 mL | 0.6322 mL | 1.2643 mL | 3.1609 mL | |
| 30 mM | 0.1054 mL | 0.5268 mL | 1.0536 mL | 2.6340 mL | |
| 40 mM | 0.0790 mL | 0.3951 mL | 0.7902 mL | 1.9755 mL | |
| 50 mM | 0.0632 mL | 0.3161 mL | 0.6322 mL | 1.5804 mL | |
| 60 mM | 0.0527 mL | 0.2634 mL | 0.5268 mL | 1.3170 mL | |
| 80 mM | 0.0395 mL | 0.1976 mL | 0.3951 mL | 0.9878 mL | |
| 100 mM | 0.0316 mL | 0.1580 mL | 0.3161 mL | 0.7902 mL |
Navoximod 関連分類
HY-18770B 関連分類
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