Bulk Inquiry
CPI-444
- Ciforadenant - V 81444- Optical Purity: 100% e.e.
- Soluble in DMSO
- MF: C20H21N7O3
- MW: 407.43
Description
CPI-444 is potent, selective and oral A2A adenosine receptor (A2aR) antagonist inhibitor (Ki value of 3.5 nM) which has demonstrated high selectivity and ability to block A2aR in in vitro studies. CPI-444 dramatically enhances immunologic responses in models of checkpoint therapy and ACT in cancer. Moreover, CPI-444 induces antitumor responses and augments efficacy to anti-PD-(L)1 and anti-CTLA-4 in preclinical models.
More Information
| Parent CAS No. | 1202402-40-1 |
|---|---|
| Chemical Name | (S)-7-(5-Methylfuran-2-yl)-3-((6-((tetrahydrofuran-3-yloxy)methyl)pyridin-2-yl)methyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine |
| SMILES | C12N=NN(CC3C=CC=C(CO[C@H]4CCOC4)N=3)C=1N=C(N)N=C2C1=CC=C(C)O1 |&1:12,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C20H21N7O3/c1-12-5-6-16(30-12)17-18-19(24-20(21)23-17)27(26-25-18)9-13-3-2-4-14(22-13)10-29-15-7-8-28-11-15/h2-6,15H,7-11H2,1H3,(H2,21,23,24)/t15-/m0/s1 |
| InChiKey | KURQKNMKCGYWRJ-HNNXBMFYSA-N |
| CID | 44537963 |
| Short Description | A2A antagonist |
References
- S Willingham et al. The adenosine A2A receptor antagonist CPI-444 blocks adenosine-mediated T-cell suppression and exhibits antitumor activity alone and in combination with anti-PD-1 and anti-PD-L1. AACR Annual Meeting 2016. Cancer Res 76:Abstract 2337
- RD Leone et al. Inhibition of the adenosine A2a receptor modulates expression of T cell co-inhibitory receptors and improves effector function for enhanced checkpoint blockade and ACT in murine cancer models. Cancer Immunol Immunother. 2018 Aug;67(8):1271-1284.
- SB Willingham et al. 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. 2018 Oct;6(10):1136-1149.
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