常見問題列表
生物活性
T-2513 是一種選擇性的拓撲異構酶 I (topoisomerase I) 抑制劑。T-2513 與拓撲異構酶 I-DNA 復合物共價結合并使其穩(wěn)定，且抑制 DNA 復制和 RNA 合成，最終導致細胞死亡。靶點
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Topoisomerase I
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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. |