Etrumadenant
Based on 9 publication(s) in Google Scholar
Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.67%
- No. CAS: 2239273-34-6
- Fòrmula: C23H22N8O
- Peso molecular:426.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Etrumadenant
More- J Exp Clin Cancer Res. 2022 Oct 14;41(1):302. [Abstract]
- Sci Signal. 2026 Mar 3;19(927):eadz6443. [Abstract]
- Commun Chem. 2023 Jun 1;6(1):106. [Abstract]
- Cells. 2024 Jun 29;13(13):1128. [Abstract]
- PLoS One. 2024 Jun 5;19(6):e0301223. [Abstract]
- bioRxiv. 2025 Jul 26:2025.07.22.666143. [Abstract]
- bioRxiv. 2024 Dec 21:2024.12.21.628442. [Abstract]
- Patent. US20230159541A1.
- Research Square Print. 2023 Feb 27.
Ver todos los productos específicos de isoformas Adenosine Receptor
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Actividad biológica
A2aR/A2bR[1]
In human in vitro cell cultures, moDC differentiated in the presence of adenosine showed a decreased ability to stimulate IFN-γ secretion from allogenic CD4+ T-cells in a MLR. This suppression is significantly reversed by addition of Etrumadenant. Multiplexed gene expression profiling using NanoString identified a cassette of 39 genes that are regulated by adenosine during moDC differentiation. Etrumadenant shows rescue of these gene expression changes[2].
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2239273-34-6
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Appearance Solid
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Peso molecular 426.47
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Fòrmula C23H22N8O
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Color Off-white to light yellow
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SMILES
N#CC1=CC=CC(C2=NC(N)=NC(C3=CN(CC4=NC(C(C)(O)C)=CC=C4)N=N3)=C2)=C1C
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Synonyms
AB928
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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J Exp Clin Cancer Res
Overcoming high level adenosine-mediated immunosuppression by DZD2269, a potent and selective A2aR antagonist. [Abstract]2022 Oct 14;41(1):302. PMID: 36229853 -
Sci Signal
Glucose metabolism sustains aberrant STAT3 signaling in colorectal cancer through glycosylated local signaling factors. [Abstract]2026 Mar 3;19(927):eadz6443. PMID: 41774818 -
Commun Chem
Crystal structure of adenosine A2A receptor in complex with clinical candidate Etrumadenant reveals unprecedented antagonist interaction. [Abstract]2023 Jun 1;6(1):106. PMID: 37264098 -
Cells
Inhibition of Vascular Smooth Muscle Cell Proliferation by ENPP1: The Role of CD73 and the Adenosine Signaling Axis. [Abstract]2024 Jun 29;13(13):1128. PMID: 38994980 -
PLoS One
Discovery of a potent, selective, and tumor-suppressing antibody antagonist of adenosine A2A receptor. [Abstract]2024 Jun 5;19(6):e0301223. PMID: 38837964 -
bioRxiv
Glucose Metabolism Sustains Aberrant STAT3 Signaling in Colorectal Cancer via Glycosylated Paracrine Factors. [Abstract]2025 Jul 26:2025.07.22.666143. PMID: 40777356 -
bioRxiv
2024 Dec 21:2024.12.21.628442. PMID: 39764043 -
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Solvente y solubilidad
DMSO : 250 mg/mL (586.21 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (4.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3448 mL | 11.7242 mL | 23.4483 mL | 58.6208 mL |
| 5 mM | 0.4690 mL | 2.3448 mL | 4.6897 mL | 11.7242 mL | |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8621 mL | |
| 15 mM | 0.1563 mL | 0.7816 mL | 1.5632 mL | 3.9081 mL | |
| 20 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL | 2.9310 mL | |
| 25 mM | 0.0938 mL | 0.4690 mL | 0.9379 mL | 2.3448 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7816 mL | 1.9540 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4655 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1724 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9770 mL | |
| 80 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL |
Etrumadenant Related Classifications
HY-129393 Related Classifications
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