CGS 15943

生物活性靶点体外研究 CGS 15943 试剂级价格

CGS 15943

CAS号:104615-18-1
英文名:CGS 15943
中文名:CGS 15943
CBNumber:CB3351424
分子式:C13H8ClN5O
分子量:285.69
MOL File:104615-18-1.mol

CGS 15943化学性质

熔点 :278-279 °C
密度 :1.72±0.1 g/cm3(Predicted)
储存条件 :room temp
溶解度 :DMSO: >16 mg/mL
酸度系数(pKa) :1.23±0.30(Predicted)
形态 :solid
颜色 :white

安全信息

WGK Germany :3

CGS 15943性质、用途与生产工艺

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。

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