Adenosine receptor antagonist 6
Adenosine receptor antagonist 6 is an orally active and selective A2A adenosine receptor (A2AAR) antagonist, with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.
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- CAS No.: 2913578-04-6
- Formula: C18H16N6O
- Molecular Weight:332.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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All Adenosine Receptor Isoforms
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Biological Activity
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A1 392.23 nM (Ki) |
A2B 2129 nM (Ki) |
A3 9036 nM (Ki) |
Adenosine receptor antagonist 6 (Compound 11a) (0.001-100 μM) exhibits dose-dependent inhibition of 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production with an IC50 of 0.089 μM in activated primary human PBMCs[1].
Adenosine receptor antagonist 6 (0.1-10 μM) abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release in activated primary human PBMCs [1].
Adenosine receptor antagonist 6 (0.03-3 μM) inhibits the NECA-mediated immunosuppression and restores the secretion of IL-2 and IFN-γ in activated primary human PBMCs [1].
Adenosine receptor antagonist 6 (0.8125-50 μM, 48 h) inhibits the proliferation of HCT116 cells (IC50 = 17.21 μM), MDA-MB-231 cells (IC50 = 53.77 μM), MC38 cells (IC50 = 18.91 μM), and CT26 cells (IC50 = 19.36 μM)[1].
Adenosine receptor antagonist 6 exhibits lower metabolic clearance by CYP450 enzymes, with CYP1A2 playing a major role in their stereoselective metabolism[1].
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.
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Animal Model:CT26 cancer cells (5 × 105 in 100 μL) were injected subcutaneously into both flanks of BALB/c mice[1]
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Dosage:25 mg/kg
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Administration:p.o. once daily for 19 days
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Result:Demonstrated a tumor growth inhibition rate (TGI) of 37%.
Exhibited significant enhancement of efficacy (TGI = 92%) when combined with PD-L1 monoclonal antibody (10 mg/kg, i.p., b.i.w.).
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Animal Model:MC38 cancer cells (5 × 105 in 100 μL) were injected subcutaneously into both flanks of C57BL/6 mice[1]
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Dosage:15 mg/kg
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Administration:p.o. once daily for 21 days
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Result:Demonstrated a tumor growth inhibition rate (TGI) of 69.74%.
Exhibited significant enhancement of efficacy (TGI = 98.1%) when combined with PD-L1 monoclonal antibody (10 mg/kg, i.p., b.i.w.).
Chemical Information
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CAS No. 2913578-04-6
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Molecular Weight 332.36
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Formula C18H16N6O
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SMILES
O=C(C1=CN2C3=CC=CC=C3N=C2C(N)=N1)N[C@@H](C)C4=NC=CC=C4
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Adenosine receptor antagonist 6 Related Classifications
HY-175195 Related Classifications
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