GIMATECAN

中文名称:

GIMATECAN

中文同义词:

吉马替康

英文名称:

ST1481

英文同义词:

CPT 184;LBQ707; ST1481; CPT 184;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

CAS号:

292618-32-7

分子式:

C25H25N3O5

分子量:

447.49

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

沸点 

780.6±70.0 °C(Predicted)

密度 

1.37±0.1 g/cm3(Predicted)

酸度系数(pKa)

11.20±0.20(Predicted)

生物活性

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。

靶点

Topoisomerase I

Topoisomerase I

体外研究

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.

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.

体内研究

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.

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.