TAS 103
| 中文名称 | TAS 103 |
|---|---|
| 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 |
| 英文名称 | TAS 103 |
| 英文同义词 | TAS 103;6-[[2-(Dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one;TAS-103 HC1;TA103(bms-247615);BMS-247615;TAS-103(salt);TAS-103 base;CS-1287 |
| CAS号 | 174634-08-3 |
| 分子式 | C20H19N3O2 |
| 分子量 | 333.38 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 174634-08-3.mol |
| 结构式 |  |
TAS 103 性质
| 熔点 | 216-217 °C(Solv: ethanol (64-17-5)) |
|---|---|
| 沸点 | 589.5±50.0 °C(Predicted) |
| 密度 | 1.350±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 7.88±0.20(Predicted) |
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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.