T-2513
Names
[ CAS No. ]:
288247-87-0
[ Name ]:
T-2513
Biological Activity
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C25H27N3O5
[ Molecular Weight ]:
449.49900
[ Exact Mass ]:
449.19500
[ PSA ]:
116.67000
[ LogP ]:
3.06990
Safety Information
[ Hazard Codes ]:
Xi