| Bioactivity | 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. [1][2]. | ||||||||||||
| Invitro | 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]. Cell Viability Assay[3] Cell Line: | ||||||||||||
| Name | CGS 15943 | ||||||||||||
| CAS | 104615-18-1 | ||||||||||||
| Formula | C13H8ClN5O | ||||||||||||
| Molar Mass | 285.69 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Gao Y, et al. CGS 15943, an adenosine A2 receptor antagonist, reduces cerebral ischemic injury in the Mongolian gerbil. Life Sci. 1994;55(3):PL61-5. [2]. Klotz KN, et al. Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):382-91. [3]. Edling CE, et al. Caffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-kinase/Akt pathway. Cancer Biol Ther. 2014 May;15(5):524-32. |
CGS 15943
CAS: 104615-18-1 F: C13H8ClN5O W: 285.69
CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Ad
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