GIMATECAN
| 中文名称 | GIMATECAN |
|---|---|
| 中文同义词 | 吉马替康;化合物 T21319 |
| 英文名称 | ST1481 |
| 英文同义词 | GIMATECAN;ST1481;ST1481: GIMATECAN;(4S)-11-((E)-((1,1-Dimethylethoxy)imino)methyl)-4-ethyl-4-hydroxy-1,12-dihydro-14H-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H)-dione;1H-Pyrano(3',4':6,7)indolizino(1,2-B)quinoline-11-carboxaldehyde, 4-ethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-, 11-(o-(1,1-dimethylethyl)oxime), (C(E),4S)-;7-T-Butoxyiminomethylcamptothecin;Lbq707;Unii-7kks9R192f |
| CAS号 | 292618-32-7 |
| 分子式 | C25H25N3O5 |
| 分子量 | 447.488 |
| EINECS号 | |
| 相关类别 | 植物提取物;标准品 -中药标准品 |
| Mol文件 | 292618-32-7.mol |
| 结构式 |  |
GIMATECAN 性质
| 沸点 | 780.6±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.37±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 酸度系数(pKa) | 11.20±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
Gimatecan (ST1481) 是一种有效的拓扑异构酶 I (topoisomerase I) 抑制剂。Gimatecan 是一种具有口服活性的喜树碱类似物。具有抗肿瘤活性。
|
Topoisomerase I
|
Gimatecan (3 to 300 ng/mL) significantly inhibits the growth of human bladder cancer models (HT1376 and MCR), thus reflecting antiproliferative potency.
Gimatecan causes a persistent S-phase arrest At 0.003 µg/mL and the number of S-phase cells increased after treatment with a higher concentration (0.03 µg/mL).
Cell Proliferation Assay
| Cell Line: | HT1376 cells harbor a p53 mutation; MCR cells harbor two p53 mutations: one in exon 4 (CGC→CCC) and one in exon 9 (CAG→TAG) |
| Concentration: | 3 to 300 ng/mL |
| Incubation Time: | 1, 6, and 24 hours |
| Result: |
IC
50
s of 90±3 and 9.0±0.4 ng/mL for MCR and HT1376 cells after treatment for 1 hours.
IC 50 s of 5.0±0.2 and 2.8±0.1 ng/mL for MCR and HT1376 cells after treatment for 24 hours. The growth-inhibitory effect was dose-dependent and time-dependent. HT1376 cells were more sensitive than MCR cells at least following a short-term exposure. |
Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth.
| Animal Model: | Athymic Swiss nude mice bearing HT1376 model |
| Dosage: | 2 mg/kg |
| Administration: | Treatment per os, every fourth day for four times |
| Result: | Caused a marked tumor growth inhibition during treatment. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-B0063 | Gimatecan | 1 mg | 1400元 | |
| 2024/04/30 | HY-B0063 | GIMATECAN Gimatecan | 292618-32-7 | 10 mg | 5800元 |