中文名称:
6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮二盐酸盐
中文同义词:
6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮二盐酸盐;拓扑异构酶I和II抑制剂(TAS-103双盐酸盐);TAS-103(BMS-247615)盐;TAS-103双盐酸盐
英文同义词:
TAS-103 (dihydrochloride);TAS-103(2HCl);TAS-103(BMS-247615);6-[[2-(Dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one dihydrochloride;BMS-247615-2HCl;BMS 247615 dihydrochloride;BMS247615 dihydrochloride;BMS-247615 dihydrochloride
储存条件
Inert atmosphere,2-8°C
生物活性
TAS-103 dihydrochloride 是一种 DNA 拓扑异构酶 I/II (topoisomerase I/II) 双重抑制剂，可用于癌症研究。
靶点
Topoisomerase I
Topoisomerase II
Topoisomerase I
Topoisomerase II
体外研究
TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC 50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103. TAS-103 inhibits the viability of HeLa cells, with an IC 50 of 40 nM. TAS-103 (10 μM) disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation.
体内研究
TAS-103 (30 mg/kg, i.v.) causes significant tumor growth suppression in mice bearing Lewis lung carcinoma (LLC) cells, without obvious body weight loss, and the liposomal TAS-103 is more active than free TAS-103.
