T-2513

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T-2513 

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。

T-2513

T-2513 Chemical Structure

CAS No. : 288247-87-0

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生物活性

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].

IC50 & Target[1]

Topoisomerase I

 

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

T-2513 (1-100 mg/kg) shows Antitumor Activity against Walker-256 carcinoma[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats bearing Walker-256 carcinoma[2]
Dosage: 1, 10, and 100 mg/kg
Administration:
Result: The ED50 was 23 mg/kg.

分子量

449.50

Formula

C25H27N3O5
CAS 号

288247-87-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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