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Ciforadenant (CPI-444) Adenosine Receptor antagonist

Name: Ciforadenant (CPI-444)
Brand: Selleck Chemicals
SKU: S6646
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S6646

Ciforadenant (CPI-444, V81444) is a potent and selective Adenosine A2A receptor antagonist. It binds to A2A receptors with a Ki of 3.54 nmol/L and demonstrates a greater than 50-fold selectivity for the A2A receptor over other adenosine receptor subtypes.

Chemical Structure

Molecular Weight: 407.43

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Adenosine Receptor Inhibitors	Reversine CGS 21680 HCl ZM241385 SCH58261 A2AR antagonist 1 Etrumadenant (AB928) Imaradenant (AZD4635) DPCPX SCH-442416 Namodenoson (CF-102)

Solubility

In vitro
Batch:

DMSO : 81 mg/mL (198.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (12.27mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (6.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	407.43	Formula	C₂₀H₂₁N₇O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1202402-40-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	V81444			SMILES	CC1=CC=C(O1)C2=C3C(=NC(=N2)N)N(N=N3)CC4=NC(=CC=C4)COC5CCOC5

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	A2AR 3.54 nM(Ki)
In vitro	CPI-444 restores T-cell activation in vitro.
In vivo	CPI-444 treatment resulted in a similar inhibition of tumor growth in the B16F10 melanoma (100 mg/kg) and RENCA renal cell cancer syngeneic models (10 mg/kg). It enhances T-cell activation in both the periphery and tumor microenvironment.
References	[1] https://pubmed.ncbi.nlm.nih.gov/30131376/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-16)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05501054	ACTIVE_NOT_RECRUITING	Renal Cell Carcinoma	M.D. Anderson Cancer Center	2023-02-09	PHASE1; PHASE2
NCT03337698	TERMINATED	Carcinoma, Non-Small-Cell Lung	Hoffmann-La Roche	2017-12-27	PHASE1; PHASE2
NCT03454451	COMPLETED	Non-Small Cell Lung Cancer; Renal Cell Cancer; Colorectal Cancer; Triple Negative Breast Cancer; Cervical Cancer; Ovarian Cancer; Pancreatic Cancer; Endometrial Cancer; Sarcoma; Squamous Cell Carcinoma of the Head and Neck; Bladder Cancer; Metastatic Castration Resistant Prostate Cancer; Non-hodgkin Lymphoma	Corvus Pharmaceuticals, Inc.	2018-04-25	PHASE1
NCT04280328	COMPLETED	Multiple Myeloma	Corvus Pharmaceuticals, Inc.	2020-02-20	PHASE1
NCT02655822	COMPLETED	Renal Cell Cancer; Metastatic Castration Resistant Prostate Cancer	Corvus Pharmaceuticals, Inc.	2016-01	PHASE1
NCT03237988	COMPLETED	Healthy Subjects	Corvus Pharmaceuticals, Inc.	2017-07-20	PHASE1

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