Brevilin A 是一种具有口服活性的STAT3/JAK抑制剂 (STAT3IC50= 10.6 μM)。Brevilin A 表现出抗肿瘤活性，对癌细胞有抗增殖活性，并能诱导细胞凋亡和自噬。
| 生物活性 | Brevilin A is an orally activeSTAT3/JAKinhibitor (STAT3IC50= 10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity tocancercells, and can induceapoptosisandautophagy[1][2]. |
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体外研究
(In Vitro) | Brevilin A (1-20 μM; 24 h) inhibits STAT3 signaling in a dose dependent manner[1].
Brevilin A (0-50 μM; 24-72 h) inhibits the proliferation of NPC cells[2].
Brevilin A (10 μM; 24 and 48 h) induces DU145 and MDA-MB-468 apoptosis after 24 h treatment[1].
Brevilin A (12.5 and 25 μM; 24 h) blocks STAT3 tyrosine 705 phosphorylation in A549R cells[1].
Cell Viability Assay[1] | Cell Line: | A549R cells | | Concentration: | 1-20 μM | | Incubation Time: | 24 hours | | Result: | Exhibited STAT3 signaling inhibition in a dose dependent manner with IC50value of 10.6 μM. |
Cell Proliferation Assay[2] | Cell Line: | CNE-2 cells | | Concentration: | 0-50 μM | | Incubation Time: | 24, 48, and 72 hours | | Result: | Showed IC50values in CNE-2 cells with treatment times of 24, 48, and 72 h of 7.93, 2.60, and 22.26 μM, respectively. |
Apoptosis Analysis[1] | Cell Line: | DU145 and MDA-MB-468 cells | | Concentration: | 10 μM | | Incubation Time: | 24 and 48 hours | | Result: | Decreased c-Myc and CyclinD1 after 24 h and 48 h treatment, increased cleaved PARP after 24 h treatment. |
Western Blot Analysis[1] | Cell Line: | A549R cells | | Concentration: | 12.5 and 25 μM | | Incubation Time: | 24 hours | | Result: | Inhibits STAT3 phosphorylation in A549R cells. |
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体内研究
(In Vivo) | Brevilin A (oral gavage; 10 and 20 mg/kg; once daily; 16 d) inhibits CNE-2 xenograft tumor growth, and inhibits PI3K/AKT and STAT3 signaling in vivo[2].
| Animal Model: | Male BALB/c nude mice injected with CNE-2 cells[2] | | Dosage: | 10 and 20 mg/kg | | Administration: | Oral gavage; 10 and 20 mg/kg; once daily; 16 days | | Result: | Decreased average tumor volumes and weights treated with 20 mg/kg by 36.3% and 46.0%, respectively, compared to vehicle control.
Inhibited the protein expression of p-AKT and p-STAT3 at both low and high doses. |
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| 来源 | - Plants
- Compositae
- Centipeda minima
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(288.67 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8867 mL | 14.4333 mL | 28.8667 mL | | 5 mM | 0.5773 mL | 2.8867 mL | 5.7733 mL | | 10 mM | 0.2887 mL | 1.4433 mL | 2.8867 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。-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: ≥ 10 mg/mL (28.87 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (28.87 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 100.0 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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 6.25 mg/mL (18.04 mM); Clear solution
此方案可获得 ≥ 6.25 mg/mL (18.04 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 62.5 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 6.25 mg/mL (18.04 mM); Clear solution
此方案可获得 ≥ 6.25 mg/mL (18.04 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 62.5 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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