Cyasterone，一种天然的EGFR抑制剂，主要分离自Ajuga decumbensThunb (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。
| 生物活性 | Cyasterone, a naturalEGFRinhibitor, mainly isolated fromAjuga decumbensThunb (Labiatae). Cyasterone manifests anti-proliferation effect by inducedapoptosisand cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors[1]. |
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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 IC50values 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].
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. |
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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].
| 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. |
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| 来源 | - Plants
- Labiatae
- Ajuga decumbensThunb.
- Plants
- Amaranthaceae
- Achyranthes bidentata
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| 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 | 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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本网站选购。 |
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