CGS-15943

CGS-15943 is a research-stage small molecule compound that acts as a potent, non-selective adenosine receptor antagonist. Developed by Ciba-Geigy, it belongs to the triazoloquinazoline chemical class and represents one of the first adenosine receptor antagonists discovered that is not a xanthine derivative. Because of this, CGS-15943 does not inhibit phosphodiesterase, offering a more specific pharmacological profile compared to traditional xanthine-based antagonists like caffeine. It is orally bioavailable and active in vivo, binding to the adenosine A1, A2A, A2B, and A3 receptors with high affinity. Additionally, CGS-15943 has been shown to inhibit the catalytic subunit of the class IB PI3K isoform p110γ. It has been investigated in preclinical research for various conditions, including pancreatic ductal adenocarcinoma, hepatocellular carcinoma, cholangiocarcinoma, estrogen receptor-positive (ER+) breast cancer, and cerebral ischemia, and has also demonstrated activity as a bone morphogenetic protein 4 (BMP-4) mimetic to stimulate osteogenic differentiation.

Other names

9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amineCGS 15943CGS15943CGS-15943CGS 15943ACGS15943ACGS-15943A