DMU-212 是一种白藜芦醇 (HY-16561) 甲基化衍生物，具有抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。DMU-212 通过诱导凋亡 (apoptosis) 和激活ERK1/2蛋白导致有丝分裂停止。DMU-212 具有口服活性。
| 生物活性 | DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant andapoptosispromoting activities. DMU-212 induces mitotic arrest via induction ofapoptosisand activation ofERK1/2protein. DMU-212 has orally active[1][2]. |
体外研究
(In Vitro) | DMU-212 (0.3125-40 μM) inhibits growth of A375, MeWo, Bro and M5 human melanoma cells[1].
DMU-212 (30-50 μM; 24 hours) induces upregulation of cell cycle inhibitors, apoptosis and ERK activation in A375 cells[1].
Cell Proliferation Assay[1] | Cell Line: | A375 cells, MeWo cells, M5 cells, Bro cells | | Concentration: | 0.3125 μM, 0,625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM | | Incubation Time: | 96 hours | | Result: | Inhibited the cellular proliferation of human melanoma cells at submicromolar or micromolar concentrations (IC50=0.5 μM for A375 and Bro and IC50= 1.25 μM for MeWo and M5 cells). |
Cell Cycle Analysis[1] | Cell Line: | A375 cells | | Concentration: | 20 μM, 30 μM, 50 μM | | Incubation Time: | 24 hours | | Result: | Caused a marked increase in the levels of p21, p53 and cyclin B1 proteins with a concomitant decrease in the levels of cyclin A2. |
Western Blot Analysis[1] | Cell Line: | A375 cells | | Concentration: | 20 μM, 30 μM, 50 μM | | Incubation Time: | 24 hours | | Result: | Significant upregulated Bax, caspase 3 and caspase 9 protein levels, while decreased the levels of the anti-apoptotic protein Bcl-2. |
Apoptosis Analysis[1] | Cell Line: | A375 cells | | Concentration: | 10 μM, 20 μM | | Incubation Time: | 24 hours, 36 hours | | Result: | Induced apoptosis. |
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体内研究
(In Vivo) | DMU-212 (50 mg/kg; i.g.; three times a week; for 14 days) inhibits tumor growth in xenograft model of human ovarian cancer[2].
| Animal Model: | 6-weeks-old SCID female mice (20-24 g), with ovarian cancer xenografts[2] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage, three times a week, for 14 days | | Result: | Lowered tumor burden. |
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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 : 20 mg/mL(66.59 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.3294 mL | 16.6472 mL | 33.2945 mL | | 5 mM | 0.6659 mL | 3.3294 mL | 6.6589 mL | | 10 mM | 0.3329 mL | 1.6647 mL | 3.3294 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%corn oil Solubility: ≥ 2 mg/mL (6.66 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (6.66 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 20.0 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。 |
