T20198 |
3,4,5,4'-四甲氧基二苯乙烯 |
MedMol | 98% |
- 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
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)