Chemical Property of (S)-7-(5-Methyl-furan-2-yl)-3-[6-(tetrahydro-furan-3-yloxyMethyl)-pyridin-2-ylMethyl]-3H-[1,2,3]triazolo[4,5-d]pyriMidin-5-ylaMine
Chemical Property:
- Melting Point:169-171°C
- Boiling Point:676.9±65.0 °C(Predicted)
- PKA:4.05±0.30(Predicted)
- Density:1.55±0.1 g/cm3(Predicted)
- Storage Temp.:-20°C
- Solubility.:Soluble in DMSO (up to at least 25 mg/ml)
- Purity/Quality:
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99%, *data from raw suppliers
CPI-444 *data from reagent suppliers
Safty Information:
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- MSDS Files:
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Useful:
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Description
CPI-444 (1202402-40-1) is a potent (Ki = 3.54 nM) and selective adenosine A2A receptor antagonist. It blocked the induction of cAMP induced by NECA in HEK-293 cells with an IC50 = 17.03 nM. CPI-444 monotherapy or in combination with anti-PD-1, anti-PD-L1, and anti-CTLA-4 induced T-cell-mediated tumor responses, inhibited tumor growth, and enabled antitumor immune memory. Currently in clinical trials for multiple cancers.
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Uses
CPI-444 is an orally administered antagonist to the A2A receptor, and binds to adenosine receptors on the surface of immune cells.
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Biological Functions
CPI-444 is a small molecule, oral, checkpoint inhibitor designed to disable a tumor’s ability to subvert attack by the immune system by blocking the binding of adenosine in the tumor microenvironment to the A2A receptor. Adenosine, a metabolite of ATP (adenosine tri-phosphate), is produced within the tumor microenvironment where it may bind to the adenosine A2A receptor present on immune cells and block their activity. CD39 and CD73 are enzymes on the surface of tumor cells and immune cells. These enzymes work in concert to convert ATP to adenosine. In vitro and preclinical studies have shown that dual blockade of CD73 and the A2A receptor may be synergistic.
