CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its K_i for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. ^[1][2]. In Vitro: CGS 15943 inhibits the kinase activity of the class IB PI3K isoform p110γ with an IC₅₀ of 1.1 μM and shows slight inhibition on p110δ with an IC₅₀ of 8.47 μM^[3].
CGS 15943 (0-20 μM; 72 hours) inhibits growth of HLF and SK-Hep-1 cells, as well as HepG2 and PLC-PRF-5 cells^[3].
CGS 15943 (0-20 μM; 24 hours) reduces the phosphorylation of Akt at its residues Ser473 and Thr308 in HLF and Sk-Hep-1 cells^[3].