522650-83-5
中文名稱
SW-044248
CAS
522650-83-5
分子式
C22H23N5O2S
分子量
421.52
MOL 文件
522650-83-5.mol
更新日期
2024/12/23 09:08:08
522650-83-5 結(jié)構(gòu)式
基本信息
中文別名
化合物SW044248TOP1抑制劑(SW044248)
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
英文別名
CS-2302SW-044248
SW-044248, >98%
SW 044248
SW044248
SW044248 >=98% (HPLC)
2-(5-ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)-N-(2-methoxyphenyl)butanamide
Butanamide, 2-[(5-ethyl-5H-1,2,4-triazino[5,6-b]indol-3-yl)thio]-N-(2-methoxyphenyl)-
2-(5-Ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-ylsulfanyl)-N-(2-methoxy-phenyl )-butyramide
常見(jiàn)問(wèn)題列表
生物活性
SW-044248是非經(jīng)典的Topo1抑制劑，對(duì)非小細(xì)胞肺癌細(xì)胞具有選擇性毒性作用。靶點(diǎn)
| Target | Value |
|
Topo1
() |
體外研究
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.