Doxycycline 是一种具有口服活性的四环素抗生素,是广谱的金属蛋白酶 (MMP) 抑制剂,具有抗菌活性和抗癌细胞增殖活性。
生物活性 | Doxycycline, anantibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1]. Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity[1][2][3][4][5]. |
IC50& Target | |
体外研究 (In Vitro) | Doxycycline (0.01-10 μg/mL, 4 d) affects growth of glioma cells only under high concentrations[2]. Doxycycline (0.01-10 μg/mL, 24 h) decreases MT-CO1 protein content with concentrations of 1 μg/mL and higher in SVG cells[2]. Doxycycline (100 ng/mL, 1 μg/mL; 24 h) reduces proliferation of human cell lines[4]. Doxycycline (0-250 μM, 72 h) inhibits cell viability of breast cancer cells[5].
Cell Viability Assay[2] Cell Line: | LNT-229, G55, and U343 glioma cells | Concentration: | 0.01, 0.1, 1 or 10 μg/mL | Incubation Time: | 4 days | Result: | Affected growth of glioma cells only under high concentration (10 μg/mL). |
Cell Viability Assay[2] Cell Line: | SVG cells | Concentration: | 0.01, 0.1, 1 or 10 μg/mL | Incubation Time: | 24 hours | Result: | Decreaseed MT-CO1 protein content with concentrations of 1 μg/mL and higher. |
Cell Proliferation Assay[4] Cell Line: | MCF 12A, 293T cells | Concentration: | 100 ng/mL, 1 μg/mL | Incubation Time: | 96 hours | Result: | Caused reduced proliferation of MCF 12A and 293T cells at 1 μg/mL. |
Cell Viability Assay[5] Cell Line: | MCF-7, MDA-MB-468 cells | Concentration: | 0-250 μM | Incubation Time: | 72 hours | Result: | Inhibited breast cancer cells in a dose-dependent manner with IC50values for MCF-7 and MDA-MB-468 of 11.39 μM and 7.13 μM respectively. |
|
体内研究 (In Vivo) | Doxycycline (oral gavage; 200 or 800 mg/kg; once daily; 3 months) reduces MMP-9 activity in untreated HT mice in a dose-dependent manner[3].
Animal Model: | 6-month-old female Heterozygous Col3a1-deficient (HT) mice[3] | Dosage: | 200 or 800 mg/kg | Administration: | Oral gavage; 200 or 800 mg/kg; once daily; 3 months | Result: | Reduced active MMP-9 in a dose-dependent manner. |
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
中文名称 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 125 mg/mL(281.26 mM;Need ultrasonic) 配制储备液 1 mM | 2.2501 mL | 11.2504 mL | 22.5007 mL | 5 mM | 0.4500 mL | 2.2501 mL | 4.5001 mL | 10 mM | 0.2250 mL | 1.1250 mL | 2.2501 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 (sealed storage, away from moisture)。-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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.68 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.68 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 *以上所有助溶剂都可在本网站选购。
|