Name | t 2513 |
---|
Description | T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death[1]. |
---|---|
Related Catalog | |
Target |
Topoisomerase I |
In Vitro | SN-38 is the metabolite of T-2513[1]. T-2513 has a broad cytotoxicity against a range of human tumor cell lines[2]. Cell Cytotoxicity Assay[2] 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 GI50s 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. |
In Vivo | T-2513 (1-100 mg/kg) shows Antitumor Activity against Walker-256 carcinoma[2]. Animal Model: Rats bearing Walker-256 carcinoma[2] Dosage: 1, 10, and 100 mg/kg Administration: Result: The ED50 was 23 mg/kg. |
References |
Molecular Formula | C25H27N3O5 |
---|---|
Molecular Weight | 449.49900 |
Exact Mass | 449.19500 |
PSA | 116.67000 |
LogP | 3.06990 |
Hazard Codes | Xi |
---|