(±)-10-Hydroxycamptothecin(Synonyms: (±)-10-HCPT)

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(±)-10-Hydroxycamptothecin (Synonyms: (±)-10-HCPT) 纯度: 99.44%

(±)-10-Hydroxycamptothecin 是一种生物碱,能够抑制拓扑异构酶 I (topoisomerase I) 的活性,具有广谱的抗肿瘤活性。

(±)-10-Hydroxycamptothecin(Synonyms: (±)-10-HCPT)

(±)-10-Hydroxycamptothecin Chemical Structure

CAS No. : 64439-81-2

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生物活性

(±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.

IC50 & Target[1]

Topoisomerase I

 

体外研究
(In Vitro)

(±)-10-Hydroxycamptothecin (10-OH-camptothecin) is an inhibitor of topo I[1]. (±)-10-Hydroxycamptothecin (10-HCPT, 5-20 nM) markedly inhibits the proliferation of Colo 205 cells in a dose-dependent manner. (±)-10-Hydroxycamptothecin (5-20 nM) arrests Colo 205 cells in the G2 phase of the cell cycle and triggers apoptosis through a caspase-3-dependent pathway[2]. (±)-10-Hydroxycamptothecin (HPT, 0.01-10 μg/mL) causes cell shrinage, nuclear fragmentation and condensed chromosomes and induces apoptosis of human urinary bladder cancer cell line (T24)[3].

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.

体内研究
(In Vivo)

(±)-10-Hydroxycamptothecin (10-HCPT, 2.5-7.5 mg/kg/2 days, p.o.) significantly suppresss tumor growth in mouse xenografts. (±)-10-Hydroxycamptothecin (1-7.5 mg/kg, p.o., once per 2 or 4 days) causes no obvious acute toxicity in nude mice[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.

分子量

364.35

Formula

C20H16N2O5

CAS 号

64439-81-2

中文名称

(±)-10-羟基喜树碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (68.62 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7446 mL 13.7231 mL 27.4461 mL
5 mM 0.5489 mL 2.7446 mL 5.4892 mL
10 mM 0.2745 mL 1.3723 mL 2.7446 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.86 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.86 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Liu SY, et al. Interaction of several nucleoside triphosphate analogues and 10-hydroxycamptothecin with human DNA topoisomerases. Cancer Res. 1989 Mar 15;49(6):1366-70.

    [2]. Ping YH, et al. Anticancer effects of low-dose 10-hydroxycamptothecin in human colon cancer. Oncol Rep. 2006 May;15(5):1273-9.

    [3]. Fan J, et al. Detection of apoptosis exposed to 10-hydroxycamptothecin in T24 human urinary bladder cancer cells. Zhonghua Wai Ke Za Zhi. 1999 Jan;37(1):57-9.

Cell Assay
[2]

Colo 205 cells (5 × 105) (ATCC: CCL-222) are seeded in 25T flasks overnight and then treated without (control) and with 5, 10, 15 or 20 nM of (±)-10-Hydroxycamptothecin, respectively. After treatment for 24-120 h, cells are harvested by trypsin-EDTA and then centrifuged at 1,500 rpm for 5 min at 4˚C. The cell pellet is resuspended in culture medium containing 0.04% trypan blue and the viable cells are enumerated by a hemocytometer[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 Administration
[2]

BALB/c-nu mice are housed in a laminar flow room under sterilized conditions with a maintained temperature of 25 ± 2˚C and a controlled 12-h light and 12-h dark cycle. The Colo 205 cells are harvested and resuspended in serum-free RPMI-1640 medium. Cells are adjusted to 1 × 107 cells/mL, and transplanted 0.1 mL subcutaneously to the flank regions of the mice. Each experimental group included six to seven mice bearing tumors. (±)-10-Hydroxycamptothecin is dissolved in propylene glycol and treatment begins when the tumor size reach 3-5 mm. (±)-10-Hydroxycamptothecin is administered via p.o. once per two or four days at doses of 1, 2.5, 5, 7.5 mg/kg (volume of injection: 0.1 mL/20 g of body weight), respectively. The control group receives propylene glycol vehicle once per two days. Tumor size and body weight are monitored twice a week throughout the experiment. The tumor size is measured using a vernier caliper. Tumor volume (V) is calculated according to the formula: V (mm3) = 0.4AB2, where A and B are the longest diameter and the shortest diameter, respectively. At the end of the experiment, all mice are sacrificed by CO2 gas. Tumors, livers, kidneys and lungs are collected, fixed, embedded and stained with hematoxylin and eosin for pathological analysis[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.

参考文献
  • [1]. Liu SY, et al. Interaction of several nucleoside triphosphate analogues and 10-hydroxycamptothecin with human DNA topoisomerases. Cancer Res. 1989 Mar 15;49(6):1366-70.

    [2]. Ping YH, et al. Anticancer effects of low-dose 10-hydroxycamptothecin in human colon cancer. Oncol Rep. 2006 May;15(5):1273-9.

    [3]. Fan J, et al. Detection of apoptosis exposed to 10-hydroxycamptothecin in T24 human urinary bladder cancer cells. Zhonghua Wai Ke Za Zhi. 1999 Jan;37(1):57-9.

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