Ciforadenant
Based on 8 publication(s) in Google Scholar
Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 1202402-40-1
- Formula: C20H21N7O3
- Molecular Weight:407.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Ciforadenant
More- Chem Eng J. 2025 Sep 29;524:168827.
- J Exp Clin Cancer Res. 2022 Oct 14;41(1):302. [Abstract]
- Sci Adv. 2023 May 5;9(18):eade5111. [Abstract]
- J Control Release. 2025 May 25:384:113889. [Abstract]
- J Med Chem. 2023 Apr 13;66(7):4734-4754. [Abstract]
- J Med Chem. 2022 Mar 10;65(5):4367-4386. [Abstract]
- Res Sq. 2026 Jun 13.
- Patent. US20230159541A1.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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IHC
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WB
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Cell Proliferation/Viability Assay
All Adenosine Receptor Isoforms
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Biological Activity
Adenosine A2A receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | EC50 |
28.5 nM
Compound: CPI-444
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Immuno-therapeutic activity in human PBMC cells assessed as restoration of NECA-inhibited IL-2 secretion by measuring recovery efficacy incubated for 24 hrs by ELISA relative to control
Immuno-therapeutic activity in human PBMC cells assessed as restoration of NECA-inhibited IL-2 secretion by measuring recovery efficacy incubated for 24 hrs by ELISA relative to control
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[PMID: 38845345] |
Ciforadenant is a potent, oral, selective A2AR antagonist. CD8+ T cell depletion abrogates the efficacy of Ciforadenant treatment as a single agent as well as in combination with anti-PD-L1, demonstrating a role for CD8+ T cells in mediating primary and secondary immune responses. Anti-tumor efficacy of Ciforadenant±anti-PD-L1 is associated with increased CD8+ cell infiltration and activation in MC38 tumor tissues, and a corresponding rise in PD-1 expression on CD8+ T cells in the spleen. Additionally, levels of immune checkpoints are modulated by treatment with Ciforadenant, including GITR, OX40, and LAG3 on tumor infiltrating lymphocytes and circulating T cells, suggesting a broad role for adenosine mediated immunosuppression[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1202402-40-1
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Appearance Solid
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Molecular Weight 407.43
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Formula C20H21N7O3
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Color White to light yellow
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SMILES
NC1=NC(C2=CC=C(C)O2)=C(N=NN3CC4=NC(CO[C@@H]5COCC5)=CC=C4)C3=N1
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Synonyms
CPI-444; V81444
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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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
Ciforadenant purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Oct 14;41(1):302. [Abstract]
The ability of A2aR antagonists (Ciforadenant (CPI-444) (10-10000 nM), ect.) to block CREB phosphorylation in CD4+ T cells was measured by flow cytometry after stimulation of whole blood with 10 µM NECA.
Ciforadenant purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Oct 14;41(1):302. [Abstract]
A2aR antagonist blocks CREB phosphorylation in CD8+T cells. Whole blood samples were incubated with A2aR antagonists (Ciforadenant (CPI-444) (10-10000 nM), ect.) for 30 minutes, then stimulated with 10 µM NECA for 15 minutes, and CREB phosphorylation in CD8+T cells was measured by flow cytometry after stimulation.
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Sci Adv
Hypoxia-inducible factor orchestrates adenosine metabolism to promote liver cancer development. [Abstract]2023 May 5;9(18):eade5111. PMID: 37146141
Ciforadenant purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 May 5;9(18):eade5111. [Abstract]
In vivo HCC tumors were induced via HDTVi of plasmids carrying Trp53KO/c-MycOE in C57BL/6N mice. (Left) Survival plot and (right) body weight of HCC-bearing mice treated with vehicle, adenosine receptor antagonists (Ciforadenant (CPI-444) (10mg/kg; oral gavage; once daily), ect.), anti–PD-1 monoclonal antibodies, or the combination of both.
Ciforadenant purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 May 5;9(18):eade5111. [Abstract]
Ciforadenant (A2AR/A2BR antagonist) (10mg/kg; oral gavage; once daily). Representative pictures and quantification of CD8+ T cells in tumor by immunohistochemistry staining.
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J Control Release
Synergistic blockade of SHP-2 and A2AR signal pathways with targeted nanoparticles restores anti-tumor immunity of CD8+ T cells. [Abstract]2025 May 25:384:113889. PMID: 40425093
Ciforadenant purchased from MedChemExpress. Usage Cited in: J Control Release. 2025 May 25:384:113889. [Abstract]
Determine time and dose of CPI-444 (Ciforadenant) (2.5-20 μM; 24-96 h) on CD8+T cell proliferation. CD8+T cells were seeded onto 96-well plate at a density of 1×106 cells per well in the complete RPMI medium containing IL-2, various concentrations of CPI-444 were added to the cells respectively, then incubated in 37℃ 5% CO2 for different time. Cell proliferation was determined using cell counting at 24, 48, 72 and 96 h.
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J Med Chem
Discovery of Pyridinone Derivatives as Potent, Selective, and Orally Bioavailable Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. [Abstract]2023 Apr 13;66(7):4734-4754. PMID: 36951370
Ciforadenant purchased from MedChemExpress. Usage Cited in: J Med Chem. 2023 Apr 13;66(7):4734-4754. [Abstract]
Ciforadenant (CPI-444) (10 μM; 30 min). The level of phosphorylated ERK in HEK293-A2AR cells evaluated by western blotting analysis. HEK293-A2AR cells were pre-incubated with different concentrations of compound 38 for 30 min and then subjected to 20 nM NECA simulation for 10 min.
Ciforadenant purchased from MedChemExpress. Usage Cited in: J Med Chem. 2023 Apr 13;66(7):4734-4754. [Abstract]
Ciforadenant (CPI-444) (10 μM; 48 h). The representative images of MC38-OVA cells co-cultured with OT-I CTL upon various treatments. Cytotoxic T lymphocytes from OT-I mouse splenocyte (OT-I CTL) were co-incubated with MC38-OVA cells for 48 h in the presence of NECA (1 μM) with or without compound 38. Then, living MC38-OVA cells were stained with a cell-permeant dye Calcein AM with green fluorescence.
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J Med Chem
Design, Synthesis, and Bioevaluation of 2-Aminopteridin-7(8 H)-one Derivatives as Novel Potent Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. [Abstract]2022 Mar 10;65(5):4367-4386. PMID: 35212542 -
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Solvent & Solubility
DMSO : 66.67 mg/mL (163.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (5.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.11 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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
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 | 2.4544 mL | 12.2720 mL | 24.5441 mL | 61.3602 mL |
| 5 mM | 0.4909 mL | 2.4544 mL | 4.9088 mL | 12.2720 mL | |
| 10 mM | 0.2454 mL | 1.2272 mL | 2.4544 mL | 6.1360 mL | |
| 15 mM | 0.1636 mL | 0.8181 mL | 1.6363 mL | 4.0907 mL | |
| 20 mM | 0.1227 mL | 0.6136 mL | 1.2272 mL | 3.0680 mL | |
| 25 mM | 0.0982 mL | 0.4909 mL | 0.9818 mL | 2.4544 mL | |
| 30 mM | 0.0818 mL | 0.4091 mL | 0.8181 mL | 2.0453 mL | |
| 40 mM | 0.0614 mL | 0.3068 mL | 0.6136 mL | 1.5340 mL | |
| 50 mM | 0.0491 mL | 0.2454 mL | 0.4909 mL | 1.2272 mL | |
| 60 mM | 0.0409 mL | 0.2045 mL | 0.4091 mL | 1.0227 mL | |
| 80 mM | 0.0307 mL | 0.1534 mL | 0.3068 mL | 0.7670 mL | |
| 100 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.6136 mL |
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