Cyasterone(Synonyms: 杯苋甾酮)

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Cyasterone (Synonyms: 杯苋甾酮) 纯度: 98.70%

Cyasterone，一种天然的 EGFR 抑制剂，主要分离自 Ajuga decumbens Thunb (Labiatae)。Cyasterone 通过诱导细胞凋亡 (apoptosis) 和细胞周期阻滞表现出抗增殖作用。 Cyasterone 可用于抗人类肿瘤的相关研究。

Cyasterone(Synonyms: 杯苋甾酮)

Cyasterone Chemical Structure

CAS No. : 17086-76-9

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生物活性

Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors[1].

IC50 & Target

IC50: EGFR[1]
体外研究
(In Vitro)

Cyasterone exerts cytotoxicity on multiple cell lines: HeLa (IC50=77.24 μg/ml); HepG-2 (IC50=52.03 μg/ml); MCF-7 (IC50=82.07 μg/ml) and MCF-7 (IC50=82.07 μg/ml). And It has none cytotoxicity (IC50>400 μg/ml) on 3 types of carcinoma (HT-29, Caco-2, T47D) and 1 type of normal (NIH 3T3) cell lines[1].
Cyasterone (0-60 μg/ml; 48 hours) causes a significantly decreasing of the cell proliferation. It inhibits cell growth as a dose-dependent manner, exhibits IC50 values of 38.50 μg/ml and 32.96 μg/ml, respectively[1].
Cyasterone (0-60 μg/ml; 24 hours) decreases p-EGFR, p-MEK, and p-mTOR as a dose-dependent manner in A549 cells, it affects the MAPK signaling pathway activities[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A549 cells and MGC823 cells
Concentration: 0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml
Incubation Time: 24 hours
Result: Inhibited cell proliferation as a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml
Incubation Time: 24 hours
Result: Surpressed p-EGFR, p-MEK, and p-mTOR expression.

体内研究
(In Vivo)

Cyasterone (intraperitoneal injection; 5 mg/kg, 10 mg/kg and 15 mg/kg; 21 days) has anti-proliferation effect in vivo and inhibits MGC823 cells xenografted tumor growth in vivo with few changes in body weights[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MGC823 xenograft tumor in BALB/C-nu mice[1]
Dosage: 5 mg/kg, 10 mg/kg and 15 mg/kg
Administration: Intraperitoneal injection
Result: Inhibited MGC823 xenograft tumor growth in vivo.

分子量

520.65

Formula

C29H44O8
CAS 号

17086-76-9
中文名称

杯苋甾酮
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 : 100 mg/mL (192.07 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9207 mL 9.6034 mL 19.2068 mL
5 mM 0.3841 mL 1.9207 mL 3.8414 mL
10 mM 0.1921 mL 0.9603 mL 1.9207 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。

    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
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    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玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Lu X, et al. Anti-proliferation effects, efficacy of cyasterone in vitro and in vivo and its mechanism. Biomed Pharmacother. 2016 Dec;84:330-339.

    [2]. Lu X,et al. Anti-proliferation effects, efficacy of cyasterone in vitro and in vivo and its mechanism.Biomed Pharmacother. 2016 Dec;84:330-339.

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