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CAS No.: 19685-09-7

(S)-10-羟基喜树碱 Catalog No. CSN10390

Synonyms: 10-羟基喜树碱;10-HCPT;10-Hydroxycamptothecin

(S)-10-hydroxycamptothecin is an inhibitor of DNA topoisomerase I with antitumor activity.

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400-920-2911

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技术信息

生物活性

描述(S) -10-Hydroxycamptothecin (HCPT) is a TOP I (Topoisomerase I) specific inhibitor. HCPT inhibits the growth of ESCC cells in vitro and verify its anti-tumor activity in vivo by using a patient-derived xenograft (PDX) tumor model in mice. HCPT also induced DNA damage by increasing the expression of H2A.XS139. HCPT significantly decreased the proliferation and anchorage-independent growth of ESCC (Esophageal squamous cell carcinoma) cells (KYSE410, KYSE510, KYSE30, and KYSE450). Mechanistically, HCPT inhibited the G2/M phase cell cycle transition, decreased the expression of cyclin B1, and elevated p21 expression. In addition, HCPT stimulated ESCC cells apoptosis, which was associated with elevated expression of cleaved PARP, cleaved caspase-3, cleaved caspase-7, Bax, Bim, and inhibition of Bcl-2 expression. HCPT dramatically suppressed PDX tumor growth and decreased the expression of Ki-67 and TOP I and increased the level of cleaved caspase-3 and H2A.XS139 expression. HCPT inhibited ESCC growth, arrested cell cycle progression, and induced apoptosis both in vitro and in vivo via decreasing the expression and activity of TOP I enzyme^[3]. HCPT may induce fibroblast apoptosis by regulating miR‑23b‑3p expression^[4].(S)-10-Hydroxycamptothecin (OPT), an analog of camptothecin (CPT), was found to inhibit the growth of the mouse hepatoma BW7756, when given at 1.0 mg/kg/day for 14 days. This drug inhibited the S-Phase of the tumor cells in vivo and the S and G2/M phases in vitro^[5].
参考文献

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
- 2.7446 mL
- 13.7230 mL
- 27.4460 mL
- 5 mM
- 0.5489 mL
- 2.7446 mL
- 5.4892 mL
- 10 mM
- 0.2745 mL
- 1.3723 mL
- 2.7446 mL

技术信息

CAS号

19685-09-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H16N2O5

运输

蓝冰

分子量

364.35

别名

10-羟基喜树碱;10-HCPT;10-Hydroxycamptothecin;羟基喜树碱

溶解度

DMSO	8.0 mg/mL (22.0 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water

30 mg/mL

suspension

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