288247-87-0
中文名稱
T-2513
英文名稱
1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, 9-(3-aminopropoxy)-4,11-diethyl-4-hydroxy-, (4S)-
CAS
288247-87-0
分子式
C25 H27 N3 O5
分子量
449.5
MOL 文件
288247-87-0.mol
288247-87-0 結(jié)構(gòu)式
基本信息
英文別名
T-25131H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, 9-(3-aminopropoxy)-4,11-diethyl-4-hydroxy-, (4S)-
物理化學(xué)性質(zhì)
沸點820.8±65.0 °C(Predicted)
密度1.40±0.1 g/cm3(Predicted)
酸度系數(shù)(pKa)11.21±0.20(Predicted)
常見問題列表
生物活性
T-2513 是一種選擇性的拓撲異構(gòu)酶 I (topoisomerase I) 抑制劑。T-2513 與拓撲異構(gòu)酶 I-DNA 復(fù)合物共價結(jié)合并使其穩(wěn)定，且抑制 DNA 復(fù)制和 RNA 合成，最終導(dǎo)致細胞死亡。靶點
|
Topoisomerase I
|
體外研究
SN-38 is the metabolite of T-2513.
T-2513 has a broad cytotoxicity against a range of human tumor cell lines.
Cell Cytotoxicity Assay
| Cell Line: | WiDr, HT-29, SK-BR-3, MKN-1, SK-LU-1, LX-1, KB, and HeLaS3 cells |
| Concentration: | 15.1-111.5 ng/mL |
| Incubation Time: | 24 hours |
| Result: | Exhibited cytotoxicity against a panel of human tumor cell lines with GI 50 s of 32.1, 97.6, 38.6, 15.6, 111.5, 15.1, 34.0, and 50.9 ng/mL for WiDr, HT-29, SK-BR-3, MKN-1, SK-LU-1, LX-1, KB, and HeLaS3 cells, respectively. |
體內(nèi)研究
T-2513 (1-100 mg/kg) shows Antitumor Activity against Walker-256 carcinoma.
| Animal Model: | Rats bearing Walker-256 carcinoma |
| Dosage: | 1, 10, and 100 mg/kg |
| Administration: | |
| Result: | The ED 50 was 23 mg/kg. |