292618-32-7
中文名稱
GIMATECAN
英文名稱
ST1481
CAS
292618-32-7
分子式
C25H25N3O5
分子量
447.49
MOL 文件
292618-32-7.mol
更新日期
2023/03/20 15:41:23
292618-32-7 結(jié)構(gòu)式
基本信息
中文別名
吉馬替康 英文別名
Lbq707ST1481
CPT 184
GIMATECAN
Unii-7kks9R192f
ST1481: GIMATECAN
LBQ707
ST1481
CPT 184
7-T-Butoxyiminomethylcamptothecin
7-[(E)-tert-butyloxyiminomethyl]-camptothecin
(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
物理化學(xué)性質(zhì)
沸點(diǎn)780.6±70.0 °C(Predicted)
密度1.37±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
酸度系數(shù)(pKa)11.20±0.20(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
Gimatecan (ST1481) 是一種有效的拓?fù)洚悩?gòu)酶 I (topoisomerase I) 抑制劑。Gimatecan 是一種具有口服活性的喜樹(shù)堿類似物。具有抗腫瘤活性。靶點(diǎn)
|
Topoisomerase I
|
體外研究
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. |
體內(nèi)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. |