| 产品描述: | DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active |
| 靶点: |
ERK;Apoptosis;Apoptosis; ERK |
| 体外研究: |
DMU-212 (0.3125-40 μM) 抑制 A375、MeWo、Bro 和 M5 人黑色素瘤细胞的生长。 DMU-212 (30-50 μM;24 小时) 诱导A375细胞中细胞周期抑制剂、细胞凋亡和ERK激活的上调。 Cell Proliferation Assay 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 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 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 Cell Line: A375 cells Concentration: 10 μM, 20 μM Incubation Time: 24 hours, 36 hours Result: Induced apoptosis. |
| 体内研究: |
DMU-212 (50 mg/kg;ig;每周 3 次;持续 14 天) 抑制人卵巢癌异种移植模型中的肿瘤生长。 Animal Model: 6-weeks-old SCID female mice (20-24 g), with ovarian cancer xenografts Dosage: 50 mg/kg Administration: Oral gavage, three times a week, for 14 days Result: Lowered tumor burden. |
| 参考文献: |
1. Vasilis Pericles Androutsopoulos, et al. Activation of ERK1/2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4. 2. Hanna Piotrowska, et al. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.329 ml |
16.647 ml |
33.295 ml |
| 5 mM |
0.666 ml |
3.329 ml |
6.659 ml |
| 10 mM |
0.333 ml |
1.665 ml |
3.329 ml |
| 50 mM |
0.067 ml |
0.333 ml |
0.666 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |