(S)-10-Hydroxycamptothecin(Synonyms: 10-羟基喜树碱; 10-HCPT; 10-Hydroxycamptothecin)

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(S)-10-Hydroxycamptothecin (Synonyms: 10-羟基喜树碱; 10-HCPT; 10-Hydroxycamptothecin) 纯度: 99.38%

(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) 是一种从喜树中分离的 DNA 拓扑异构酶 I (DNA topoisomerase I) 抑制剂。(S)-10-Hydroxycamptothecin 可显着诱导细胞凋亡,并可用于肝癌,胃癌,结肠癌和白血病的研究。

(S)-10-Hydroxycamptothecin(Synonyms: 10-羟基喜树碱; 10-HCPT;  10-Hydroxycamptothecin)

(S)-10-Hydroxycamptothecin Chemical Structure

CAS No. : 19685-09-7

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生物活性

(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment[1][2][3][4].

IC50 & Target[1][3]

Topoisomerase I

 

体外研究
(In Vitro)

(S)-10-Hydroxycamptothecin (5-20 µg/L; 6 days; Hep G2 cells) treatment results in the cell cycle arrest at G2/M phase[2].
(S)-10-Hydroxycamptothecin induces differentiation, down-regulates nuclear antigen (PCNA) and up-regulates wild-type protein p53 in Hep G2 cells[2].
(S)-10-Hydroxycamptothecin inhibits L1210 leukemia cells with an IC50 of 1.15 µM[1].

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 Cycle Analysis[2]

Cell Line: Hep G2 cells
Concentration: 5 µg/L, 10 µg/L, 20 µg/L
Incubation Time: 6 days
Result: Hep G2 cells were mainly arrested at G2/M phase.

体内研究
(In Vivo)

(S)-10-Hydroxycamptothecin (10-Hydroxycamptothecin) against L1210 leukemia in mice is tested. At the optimal dose (15 mg/kg), (S)-10-Hydroxycamptothecin has a 71% increase in life span (ILS)[1].

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

19685-09-7

中文名称

10-羟基喜树碱;(S)-10-羟基喜树碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (137.23 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 (protect from light)。-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    40% PEG300    5% Tween-80    45% 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 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    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]. Min Liu, et al. Intracellular delivery of 10-hydroxycamptothecin with targeted nanostructured lipid carriers against multidrug resistance . Journal of Drug Targeting.

    [2]. Min Liu, et al. Intracellular delivery of 10-hydroxycamptothecin with targeted nanostructured lipid carriers against multidrug resistance. J Drug Target, Early Online: 1–8

    [3]. Yu P, et al. Synthesis and preliminary anticancer evaluation of 10-hydroxycamptothecin analogs. Biol Pharm Bull. 2012;35(8):1295-9.

    [4]. Zhang XW, et al. Differentiation-inducing action of 10-hydroxycamptothecin on human hepatoma Hep G2 cells. Acta Pharmacol Sin. 2000 Apr;21(4):364-8.

    [5]. Zhang XW, et al. Differential regulation of P53, c-Myc, Bcl-2, Bax and AFP protein expression, and caspase activity during 10-hydroxycamptothecin-induced apoptosis in Hep G2 cells. Anticancer Drugs. 2000 Oct;11(9):747-56.

    [6]. Liu M, et al. Intracellular delivery of 10-hydroxycamptothecin with targeted nanostructured lipid carriers against multidrug resistance. J Drug Target. 2016;24(5):433-40.

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