174634-09-4
174634-09-4 结构式
基本信息
TAS-103(BMS-247615)盐
拓扑异构酶I和II抑制剂(TAS-103双盐酸盐)
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
TAS-103(2HCl)
BMS-247615-2HCl
TAS-103(BMS-247615)
TAS 103 (hydrochloride)
BMS247615 dihydrochloride
BMS-247615 dihydrochloride
BMS 247615 dihydrochloride
TAS-103 (dihydrochloride)
TAS 103 dihydrochloride, BMS 247615 dihydrochloride
物理化学性质
常见问题列表
|
Topoisomerase I
|
Topoisomerase II
|
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.
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.