GIMATECAN
|
|
|
- CAS号:
- 292618-32-7
- 英文名:
- ST1481
- 英文别名:
- ST1481;Lbq707;STI481;CPT 184;GIMATECAN;Unii-7kks9R192f;ST1481: GIMATECAN;LBQ707; ST1481; CPT 184;ST1481 ST-1481 Gimatecan;7-T-Butoxyiminomethylcamptothecin
- 中文名:
- GIMATECAN
- 中文别名:
- 吉马替康;化合物 T21319
- CBNumber:
- CB01011641
- 分子式:
- C25H25N3O5
- 分子量:
- 447.488
- MOL File:
- 292618-32-7.mol
|
|
|
GIMATECAN化学性质
-
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)
-
|
GIMATECAN性质、用途与生产工艺
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。
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.
|
GIMATECAN
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-B0063 | Gimatecan | | 1 mg | 1400元 |
| 2024/01/25 | HY-B0063 | GIMATECAN
Gimatecan | 292618-32-7 | 5mg | 3500元 |
292618-32-7, GIMATECAN 相关搜索:
- 标准品 -中药标准品
- 植物提取物
- 化合物 T21319
- 吉马替康
- 292618-32-7
- ST1481 ST-1481 Gimatecan
- STI481
- 7-[(E)-tert-butyloxyiminomethyl]-camptothecin
- LBQ707; ST1481; CPT 184
- CPT 184
- Unii-7kks9R192f
- Lbq707
- 7-T-Butoxyiminomethylcamptothecin
- 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)-
- (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
- ST1481: GIMATECAN
- ST1481
- GIMATECAN