SW-044248

中文名称:

SW-044248

中文同义词:

2-[(5-乙基-5H-1,2,4-三嗪并[5,6-B]吲哚-3-基)硫基]-N-(2-甲氧基苯基)丁酰胺;TOP1抑制剂(SW044248);化合物SW044248

英文名称:

2-(5-ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)-N-(2-methoxyphenyl)butanamide

英文同义词:

SW 044248;SW044248;CS-2302;SW-044248, >98%;2-(5-ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)-N-(2-methoxyphenyl)butanamide;SW-044248; 2-(5-Ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-ylsulfanyl)-N-(2-methoxy-phenyl )-butyramide;Butanamide, 2-[(5-ethyl-5H-1,2,4-triazino[5,6-b]indol-3-yl)thio]-N-(2-methoxyphenyl)-;SW044248 >=98% (HPLC)

CAS号:

522650-83-5

分子式:

C22H23N5O2S

分子量:

421.52

EINECS号:

相关类别:

细胞生物学试剂;抑制剂

Mol文件:

522650-83-5.mol

储存条件 

2-8°C

形态

powder

颜色

white to beige

生物活性

SW-044248是非经典的Topo1抑制剂，对非小细胞肺癌细胞具有选择性毒性作用。

靶点

Target Value Topo1 ()

Target

Value

Topo1 ()

体外研究

SW044248 is a non-canonical Top1 inhibitor, and is selectively toxic for certain NSCLC cell lines. SW044248 shows no effect on Top2. SW044248 (2, 5, 10 μM) rapidly inhibits transcription, translation and DNA synthesis in sensitive cells (HCC4017 and H292 cells) but not insensitive cells (HBEC30KT cells and HCC44 cells). SW044248 (10 μM) rapidly activates the integrated stress response through kinases GCN2 and PKR. The inhibition of Top1 in HCC4017 cells is helpful to the toxicity of SW044248. SW044248 (5, 10 μM) shows no effect on HBEC30KT and HCC44 cell lines due to the up-regulation of p21 CDKN1A . SW044248 is selectively toxic in 18/74 NSCLC lines.