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104615-18-1

中文名稱 CGS 15943
英文名稱 CGS 15943
CAS 104615-18-1
分子式 C13H8ClN5O
分子量 285.69
MOL 文件 104615-18-1.mol
更新日期 2024/11/03 13:08:37
104615-18-1 結(jié)構(gòu)式 104615-18-1 結(jié)構(gòu)式

基本信息

中文別名
化合物CGS 15943
9-氯-2-(2-呋喃基) - [1,2,4]三唑并[1,5-C]喹唑啉-5-胺
英文別名
CGS 15943
CGS-15943A
CGS-15943 solid
CGS-15943 ADENOSINE A1 RECEPTOR
9-CHLORO-2-(2-FURYL)(1,2,4)TRIAZOLO(1,5-C)QUINAZOLIN-5-AMINE
9-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine
9-Chloro-2-(furan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-amine
9-CHLORO-2-(2-FURANYL)-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE
[1,2,4]Triazolo[1,5-c]quinazolin-5-amine,9-chloro-2-(2-furanyl)-
9-Chloro-5,6-dihydro-2-(furan-2-yl)[1,2,4]triazolo[1,5-c]quinazolin-5-imine

物理化學(xué)性質(zhì)

熔點(diǎn)278-279 °C
密度1.72±0.1 g/cm3(Predicted)
儲(chǔ)存條件room temp
溶解度DMSO: >16 mg/mL
溶解度二甲基亞砜:>16 mg/mL
酸度系數(shù)(pKa)1.23±0.30(Predicted)
形態(tài)solid
顏色white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
WGK Germany3
WGK Germany3

常見問題列表

生物活性
CGS 15943 是 adenosine receptor 腺苷受體的非黃嘌呤拮抗劑,具有口服活性。接受人重組 A1,A2A,A2B和 A3 受體轉(zhuǎn)染的 CHO 細(xì)胞中,Ki 值分別為 3.5、4.2、16 和 50 nM。
靶點(diǎn)

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)

體外研究

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
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