1. GPCR/G Protein
  2. Adenosine Receptor
  3. CPI-444

CPI-444 (Synonyms: V81444; ciforadenant)

Cat. No.: HY-101978 Purity: 99.94%
Handling Instructions

CPI-444 (V81444) 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.

CPI-444 Chemical Structure

CPI-444 Chemical Structure

CAS No. : 1202402-40-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1  mL in DMSO USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses[1].

IC50 & Target

Adenosine A2A receptor[1]

In Vitro

CPI-444 is a potent, oral, selective A2AR antagonist. CD8+ T cell depletion abrogates the efficacy of CPI-444 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 CPI-444±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 CPI-444, including GITR, OX40, and LAG3 on tumor infiltrating lymphocytes and circulating T cells, suggesting a broad role for adenosine mediated immunosuppression[1].

In Vivo

Daily treatment of the syngeneic mouse model MC38 with CPI-444 (1, 10, 100 mg/kg) leads to dose-dependent inhibition of tumor growth, leading to tumor elimination in ~30% of treated mice. Combining CPI-444 (100 mg/kg, qd, 14 days) with anti-PD-L1 (200 μg, 3qw, 4 doses) treatment in MC38 models synergistically inhibits tumor growth and eliminates tumors in 90% of treated mice. When cured mice are later re-challenged with MC38 cells, tumor growth is rejected in 100% of challenged mice, indicating that CPI-444 induces systemic anti-tumor immune memory[1].

Clinical Trial
Molecular Weight

407.43

Formula

C₂₀H₂₁N₇O₃

CAS No.

1202402-40-1

SMILES

NC1=NC(C2=CC=C(C)O2)=C(N=NN3CC4=NC(CO[[email protected]@H]5COCC5)=CC=C4)C3=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 67.5 mg/mL (165.67 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4544 mL 12.2720 mL 24.5441 mL
5 mM 0.4909 mL 2.4544 mL 4.9088 mL
10 mM 0.2454 mL 1.2272 mL 2.4544 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.25 mg/mL (5.52 mM); Clear solution

  • 2.

    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

*All of the co-solvents are provided by MCE.
References

Purity: 99.94%

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Keywords:

CPI-444V81444ciforadenantCPI444CPI 444V 81444V-81444Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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Product name:
CPI-444
Cat. No.:
HY-101978
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