CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .
IC50&Target
p110γ
1.1 μM (IC50)
p110δ
8.47 μM (IC50)
adenosine A1 receptor
3.5 nM (Ki)
adenosine A2A receptor
4.2 nM (Ki)
adenosine A2B receptor
16 nM (Ki)
adenosine A3 receptor
50 nM (Ki)
体外研究
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.
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.
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.
Cell Viability Assay
Cell Line:
HLF, SK-Hep-1, HepG2 and PLC-PRF-5 cells
Concentration:
0 μM; 1 μM; 5 μM; 10 μM; 20 μM
Incubation Time:
24 hours
Result:
Inhibited growth of four distinct HCC cell lines.
Western Blot Analysis
Cell Line:
HLF and Sk-Hep-1 cells
Concentration:
0 μM; 1 μM; 5 μM; 10 μM; 20 μM
Incubation Time:
24 hours
Result:
Inhibited the PI3K/Akt pathway in HLF and Sk-Hep-1 cells
分子式
C13H8N5OCl
分子量
285.69
CAS号
104615-18-1
运输条件
Room temperature in continental US; may vary elsewhere.