174634-08-3
174634-08-3 结构式
基本信息
CS-1287
BMS-247615
TAS-103 HC1
TAS-103 base
TAS-103(salt)
TA103(bms-247615)
6-[[2-(Dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one
7H-Indeno[2,1-c]quinolin-7-one, 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-
物理化学性质
常见问题列表
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Topoisomerase I
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Topoisomerase II
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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.