288247-87-0

288247-87-0 structure
288247-87-0 structure
  • Name: T-2513
  • Chemical Name: t 2513
  • CAS Number: 288247-87-0
  • Molecular Formula: C25H27N3O5
  • Molecular Weight: 449.49900
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage DNA/RNA Synthesis
  • Create Date: 2017-10-17 10:05:26
  • Modify Date: 2024-01-10 14:21:35
  • 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].

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

[1]. Stephan A Veltkamp, et al. Clinical and pharmacologic study of the novel prodrug delimotecan (MEN 4901/T-0128) in patients with solid tumors. Clin Cancer Res. 2008 Nov 15;14(22):7535-44.

[2]. S Okuno, et al. Complete regression of xenografted human carcinomas by camptothecin analogue-carboxymethyl dextran conjugate (T-0128). Cancer Res. 2000 Jun 1;60(11):2988-95.

Molecular Formula C25H27N3O5
Molecular Weight 449.49900
Exact Mass 449.19500
PSA 116.67000
LogP 3.06990
Hazard Codes Xi
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