T-2513 hydrochloride

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CAS NO:

187793-52-8

T-2513 hydrochloride 是一种选择性的拓扑异构酶 I (topoisomerase I) 抑制剂。T-2513 hydrochloride 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。

生物活性

T-2513 hydrochloride is a selectivetopoisomeraseIinhibitor. T-2513 hydrochloride binds covalently to and stabilizes thetopoisomeraseI-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 hydrochloride^[1].
T-2513 hydrochloride has a broad cytotoxicity against a range of human tumor cell lines^[2].

Cell Viability 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 hydrochloride (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 ED₅₀was 23 mg/kg.

分子量

485.96

Formula

C₂₅H₂₈ClN₃O₅

CAS 号

187793-52-8

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.