TAS-103
TAS-103(TAS-103)
CAS: 174634-08-3
化学式: C20H19N3O2
| 中文名 | TAS-103 |
| 英文名 | TAS-103 |
| 别名 | 6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮 |
| 英文别名 | TAS 103 CS-1287 TAS-103 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 |
| CAS | 174634-08-3 |
| 化学式 | C20H19N3O2 |
| 分子量 | 333.38 |
| 密度 | 1.350±0.06 g/cm3(Predicted) |
| 熔点 | 216-217 °C(Solv: ethanol (64-17-5)) |
| 沸点 | 589.5±50.0 °C(Predicted) |
| 溶解度 | 10毫米DMSO |
| 酸度系数 | 7.88±0.20(Predicted) |
| 存储条件 | -20℃ |
| 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. |
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