CPI-444
Adenosine A2A receptor antagonist / 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.1,2 Currently in clinical trials for multiple cancers.3
Biochemicals & reagents
1202402-40-1
Ciforadenant
1) Willingham et al. (2018), A2AR Antagonism with CPI-444 Induces Antitumor Responses and Augments Efficacy to Anti-PD-(L)1 and Anti-CTLA-4 in Preclinical Models; Cancer Immunol. Res. 6 1136 2) Leone et al. (2018), ), Inhibition of the adenosine A2a receptor modulates expression of T cell coinhibitory receptors and improves effector function for enhanced checkpoint blockade and ACT in murine cancer models; Cancer Immunol. Immunother. 671271 3) NCT02655822
-20°C
TARGET: GPCR -- PATHWAY: cAMP / cGMP signaling -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer