依喜替康
| 中文名称 | 依喜替康 |
|---|---|
| 中文同义词 | 依喜替康;依喜替康杂质;伊立替康杂质36;伊喜替康;依喜替康游离态;阿依 沙替康 |
| 英文名称 | Exatecan |
| 英文同义词 | 10H,13H-BENZO[DE]PYRANO[3',4':6,7]INDOLIZINO[1,2-B]QUINOLINE-10,13-DIONE, 1-AMINO-9-ETHYL-5-FLUORO-1,2,3,9,12,15-HEXAHYDRO-9-HYDROXY-4-METHYL-, (1S,9S)-, MONOMETHANESULFONATE (SALT);(1S,9S)-1-Amino-9-ethyl-5-fluoro-1,2,3,9,12,15-hexahydro-9-hydroxy-4-methyl-10H,13H-benzo(de)pyrano(3',4':6,7)indolizino(1,2-b)quinoline-10,13-dione;Exatecan;CS-147;Exatecan Impurity;10H,13H-Benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinoline-10,13-dione, 1-amino-9-ethyl-5-fluoro-1,2,3,9,12,15-hexahydro-9-hydroxy-4-methyl-, (1S,9S)-;Irinotecan Impurity 36;1 Exatecan |
| CAS号 | 171335-80-1 |
| 分子式 | C24H22FN3O4 |
| 分子量 | 435.45 |
| EINECS号 | |
| 相关类别 | 对照品-杂质对照品;原料药;医药原料;细胞毒素;科研试剂;精细化工原料;精品科研试剂 |
| Mol文件 | 171335-80-1.mol |
| 结构式 |  |
依喜替康 性质
| 沸点 | 818.4±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.53±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C,protect from light |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 11.19±0.40(Predicted) |
|
Topoisomerase I 2.2 μM (IC 50 ) |
Exatecan is a potent topoisomerase I inhibitor, with an IC 50 of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI 50 s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively. Exatecan Mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI 50 s of 0.186 and 0.395 ng/mL, respctively. Exatecan Mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.
Exatecan Mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan Mesylate (15, 25 mg/kg, i.v.) hightly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan Mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.