CGS 15943

CGS 15943用途

CGS 15943 是一种腺苷 A2 受体 (adenosine A2 receptor) 拮抗剂,可减轻蒙古沙土鼠的中风损伤。CGS 15943 是一种选择性 p110γ 抑制剂,IC50为 1.1 μM,对 p110δ 有抑制作用 (IC50=8.47 μM),对 HCC 和 PDAC 细胞具有抗癌作用。

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CGS 15943名称

[ CAS 号 ]:
104615-18-1

[ 英文名 ]:
CGS 15943

[英文别名 ]:

MFCD01529897

CGS 15943生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> PI3K/Akt/mTOR 信号通路 >> PI3K

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

[ 靶点 ]

p110γ:1.1 μM (IC50)

p110δ:8.47 μM (IC50)

adenosine A2 receptor

[体外研究]

CGS 15943(0-20μM; 72小时)抑制HLF和SK-Hep-1细胞以及HepG2和PLC-PRF-5细胞的生长[2]。CGS 15943(0-20μM; 24小时)降低HLF和Sk-Hep-1细胞中Akt残基Ser473和Thr308的磷酸化[2]。细胞活力测定[2]细胞系：HLF,SK-Hep-1,HepG2和PLC-PRF-5细胞浓度：0μM; 1μM; 5μM; 10μM; 20μM培养时间：24小时结果：抑制四种不同HCC细胞系的生长。Western Blot分析[2]细胞系：HLF和Sk-Hep-1细胞浓度：0μM; 1μM; 5μM; 10μM; 20μM培养时间：24小时结果：抑制HLF和Sk-Hep-1细胞中的PI3K/Akt途径

[参考文献]

[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]. 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物理化学性质

[ 密度 ]:
1.72 g/cm3

[ 沸点 ]:
566.6ºC at 760 mmHg

[ 熔点 ]:
278-279 °C

[ 分子式 ]:
C₁₃H₈ClN₅O

[ 分子量 ]:
285.68900

[ 闪点 ]:
296.5ºC

[ 精确质量 ]:
285.04200

[ PSA ]:
82.24000

[ LogP ]:
3.35430

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
7.4E-13mmHg at 25°C

[ 折射率 ]:
1.84

[ 储存条件 ]:
室温

CGS 15943MSDS

详细MSDS(安全技术说明书)

CGS 15943安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

CGS 15943文献

Adenosine induces growth-cone turning of sensory neurons.

Purinergic Signal. 4(4) , 357-64, (2008)

The formation of appropriate connections between neurons and their specific targets is an essential step during development and repair of the nervous system. Growth cones are located at the leading ed...

Caffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-kinase/Akt pathway.

Cancer Biol. Ther. 15(5) , 524-32, (2014)

Caffeine is a naturally occurring methylxanthine that acts as a non-selective adenosine receptor antagonist. Epidemiological studies demonstrated habitual coffee drinking to be significantly associate...

The effect of adenosine on pro-inflammatory cytokine production by porcine T cells.

Vet. Immunol. Immunopathol. 145(1-2) , 332-9, (2012)

Adenosine is a well described anti-inflammatory modulator of immune responses. The aim of the present study was to describe the role of common adenosine agonist 5'-N-ethylcarboxamidoadenosine (NECA) i...

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