A2AR/A2BR antagonist 2
A2AR/A2BR antagonist 2 is a dual A2A/A2B adenosine receptor antagonist with selectivity for the A1 receptor. A2AR/A2BR antagonist 2 reverses adenosine-mediated T-cell immunosuppression in the tumor microenvironment. A2AR/A2BR antagonist 2 can be used in cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 2975718-45-5
- Formula: C22H26N8O
- Molecular Weight:418.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adenosine Receptor Isoforms
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Biological Activity
Description
In Vitro
A2AR/A2BR antagonist 2 (compound 34) potently inhibits recombinant A2AR (Ki = 0.3 nM, cAMP IC50 = 4.2 nM) and recombinant A2BR (cAMP IC50 = 21.1 nM), and exhibits high selectivity for recombinant A1R (Ki = 541.0 nM) with a selectivity factor of approximately 1803-fold[1].
A2AR/A2BR antagonist 2 exhibits off-target inhibitory activity against protein serine/threonine kinases (IC50 = 1 μM), as well as off-target inhibitory activity against muscarinic M1-M4 receptors (IC50 = 2-6 μM), serotonin 5-HT1B receptor (IC50 = 2 μM) and 5-HT2B receptor (IC50 = 5 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 2975718-45-5
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Molecular Weight 418.49
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Formula C22H26N8O
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SMILES
COC1=CC=CC2=C1N=C(N3N=C(N=C23)[C@H]4C[C@@H](C4)C5=C(N=C(C=N5)C(C)(N)C)C)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Multiplex immunofluorescence IHC
Multiplex immunofluorescence IHC detects multiple protein biomarkers in one tissue section by sequential antibody staining, HRP-mediated tyramide fluorophore deposition, heat-mediated antibody stripping, nuclear counterstaining, multispectral imaging, spectral unmixing, and digital cell phenotyping; TSA deposits fluorophore near the antigen so the fluorescence signal remains after primary and secondary antibodies are removed, enabling repeated staining cycles, including with antibodies from the same host species. Classic FFPE tumor immune-profiling applications use panels such as CD3, CD8, CD68/CD163, FOXP3, PD-1, PD-L1, pancytokeratin, Ki67, and DAPI to identify tumor cells, immune-cell subsets, checkpoint-marker expression, co-expression phenotypes, cell density, and spatial relationships in the tumor microenvironment.
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Multiplex immunohistochemistry
Multiplex immunohistochemistry (mIHC), also known as tyramide dignal amplification (TSA), is an enzymatic detection method that uses horseradish peroxidase (HRP) to perform high-density in-situ labeling of target proteins or nucleic acids.
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)