104615-18-1 | CGS 15943
英文名称
CGS 15943
分子式
C13H8ClN5O
分子量
285.69
结构式
中文别名
英文别名
| 属性 | 值 |
|---|---|
| 密度 | 1.72±0.1 g/cm3(Predicted) |
| 形态 | solid |
| 熔点 | 278-279 °C |
| 颜色 | white |
| 溶解度 | 二甲基亚砜：>16 mg/mL |
| 储存条件 | room temp |
| 酸度系数(pKa) | 1.23±0.30(Predicted) |
| 属性 | 值 |
|---|---|
| 警示词 | 警告 |
| WGK Germany | 3 |
| 防范说明 | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
| 危险性描述 | H302-H315-H319-H335 |
| 危险性符号(GHS) | GHS07 |
| 标题 | 内容 |
|---|---|
| 靶点 | p110γ 1.1 μM (IC 50 ) p110δ 8.47 μM (IC 50 ) adenosine A1 receptor 3.5 nM (Ki) adenosine A2A receptor 4.2 nM (Ki) adenosine A2B receptor 16 nM (Ki) adenosine A3 receptor 51 nM (Ki) |
| 体外研究 | CGS 15943 inhibits the kinase activity of the class IB PI3K isoform p110γ with an IC 50 of 1.1 μM and shows slight inhibition on p110δ with an IC 50 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 |
| 生物活性 | CGS 15943 是 adenosine receptor 腺苷受体的非黄嘌呤拮抗剂，具有口服活性。接受人重组 A1，A2A，A2B和 A3 受体转染的 CHO 细胞中，Ki 值分别为 3.5、4.2、16 和 50 nM。 |