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CAS No.: 213819-48-8

Belotecan hydrochloride/盐酸贝洛特坎 Catalog No. CSN21568

Synonyms: CKD-602;CKD-602 hydrochloride;Belotecan (hydrochloride)

Belotecan hydrochloride, a synthetic and water-soluble camptothecin derivative, is inhibitor of topoisomerase I.

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400-920-2911

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生物活性

描述Type I and type II topoisomerase inhibitors interfere with DNA 'unwinding' during DNA replication and RNA transcription. Topoisomerase I (TOP1) cuts one strand in the double-stranded DNA, independent of ATP. Belotecan HCl (CKD-602), the synthetic water-solube camptothecin analogue, a TOP1 inhibitor and has been shown to be effective in the treatment of various cancers. Treatment with belotecan showed a significant cytotoxic effect in all cervical cancer cell lines in a time- and dose-dependent manner. The IC₅₀ values were 30 ng/ml for Caski cells, 150 ng/ml for HeLa cells, and 150 ng/ml for SiHa cells at 48h after treatment. A strong pro-apoptotic activity was observed in the treatment groups after 48 h of treatment. Compared to the control, apoptosis rates significantly increased in Caski, HeLa and Siha when treated with different concentrations (half the IC₅₀ and IC₅₀ values). The treatment increased the expression of PARP (Poly(ADP-ribose) polymerase), cleaved PARP and Bcl2-associated X protein (BAX). In addition, expression of both p53 and phosphorylated p53 (Ser15) was increased. Belotecan treatment induced the G2/M phase cell accumulation in all cell lines in a concentration-dependent manner. The protein expression levels of MMP2 and VEGF, two proteins known to be specifically related to the invasive ability of cells, decreased following belotecan treatment. In vivo, treatment with belotecan (25 mg/kg; intravenously) significantly inhibited the tumor growth of this xenograft model compared with the control (p < 0.05)^[1].
参考文献

[1] Lee S, Ho JY, Liu JJ, et al. CKD-602, a topoisomerase I inhibitor, induces apoptosis and cell-cycle arrest and inhibits invasion in cervical cancer. Mol Med. 2019;25(1):23

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1278 mL
- 10.6392 mL
- 21.2784 mL
- 5 mM
- 0.4256 mL
- 2.1278 mL
- 4.2557 mL
- 10 mM
- 0.2128 mL
- 1.0639 mL
- 2.1278 mL

技术信息

CAS号

213819-48-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H28ClN3O4

运输

蓝冰

分子量

469.96

别名

CKD-602;CKD-602 hydrochloride;Belotecan (hydrochloride);7-[2-(N-isopropylamino)ethyl]-(20S)-Camptothecin;(S)-CKD602;Belotecan Hydrochloride;Camtobell;Belotecan

溶解度

DMSO	55.0 mg/mL (117.0 mM)
Water	insoluble

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Belotecan hydrochloride/盐酸贝洛特坎 Catalog No. CSN21568

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