T-2513
| 中文名称 | T-2513 |
|---|---|
| 中文同义词 | |
| 英文名称 | 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)- |
| 英文同义词 | 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)-;T-2513 |
| CAS号 | 288247-87-0 |
| 分子式 | C25 H27 N3 O5 |
| 分子量 | 449.5 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 288247-87-0.mol |
| 结构式 |  |
T-2513 性质
| 沸点 | 820.8±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.40±0.1 g/cm3(Predicted) |
| 酸度系数(pKa) | 11.21±0.20(Predicted) |
T-2513 是一种选择性的拓扑异构酶 I (topoisomerase I) 抑制剂。T-2513 与拓扑异构酶 I-DNA 复合物共价结合并使其稳定，且抑制 DNA 复制和 RNA 合成，最终导致细胞死亡。
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Topoisomerase I
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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. |
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. |