| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S87972-1mg |
98.2% | ￥200.00 | 10 | - | - | - |
|
S87972-5mg |
98.2% | ￥380.00 | 8 | - | - | - |
|
S87972-10mg |
98.2% | ￥650.00 | 6 | - | - | - |
|
S87972-25mg |
98.2% | ￥1500.00 | 6 | - | - | - |
|
S87972-50mg |
≥98% | ￥2800.00 | 货期：2-3天 | - | - | - |
|
S87972-100mg |
≥98% | ￥3800.00 | 货期：2-3天 | - | - | - |
|
FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1).
| 产品描述： | FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1). | ||||||||||||||||||||
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| 靶点： | BRD4(1):0.43 μM (IC50);EpigeneticReaderDomain | ||||||||||||||||||||
| 体外研究： | FL-411 is a selective BRD4 inhibitor. Binding affinities of FL-411 are measured by TR-FRET against the first and second bromodomains of BRD2(1), BRD4(1), and BRD4(2) with IC50s of 24.60±0.70 μM, 0.47±0.02 μM, 0.93±0.05 μM, respectively. FL-411 possesses a good BRD4(1) inhibition activity (IC50=0.43±0.09 μM), antiproliferative activity (MCF-7, IC50=1.62±0.06 μM; MDA-MB-231, IC50=3.27±0.14 μM), and autophagic activity (42.29% in MCF-7 cells), as well as displays a low toxicity against MCF10A cells). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction and thus activating AMPK-mTOR-ULK1-modulated autophagic pathway in breast cancer cells | ||||||||||||||||||||
| 体内研究： | To evaluate the antitumor activity of FL-411 in vivo, two breast tumor xenograft models, namely, MCF-7 and MDA-MB-231 cell lines models, are used. The in vivo study is conducted using three different doses of FL-411: 25 mg/kg, 50 mg/kg, and 100 mg/kg. In all the models, FL-411 shows significant tumor growth inhibition in a dose-dependent manner as determined by 80% and 76% tumor growth inhibition ratio in MCF-7 and MDA-MB-231 cell models, respectively. A remarkable loss of tumor weights is observed in all dose groups (p<0.001). FL-411 displays no obvious effects on the body weight of all the treatment groups. To examine whether FL-411-mediated inhibition of tumor growth in vivo is associated with reduced cell proliferation and the increased autophagy-associated cell death, tumor tissues from control and FL-411-treated mice are processed for the immunohistochemical analysis of Ki-67 and LC3. FL-411 treatment obviously reduces the number of Ki-67 (p<0.001) positive cells as well as increases autophagy levels, which is determined by increased LC3 expression (p<0.001) | ||||||||||||||||||||
| 参考文献： | 1. Ouyang L, et al. Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That InducesAMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer. J Med Chem. 2017 Dec 28;60(24):9990-10012. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 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。 |
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营业执照(三证合一)
北京