| 产品描述: | HIF 抑制剂;HIF Inhibitors;;InformationIDF-11774 IDF-11774 is a hypoxia-inducible factor-1 (HIF-1) inhibitor. It reduces the HRE-luciferase activity of HIF-1α (IC50 = 3.65 μM) and blocks HIF-1α accumulation under hypoxia in HCT116 human colon cancer cells.TargetsHIF-1In vitroIDF-11774 inhibits the accumulation of HIF-1α in vitro and in vivo in colorectal carcinoma HCT116 cells under hypoxic conditions. The treatment of IDF-11774 suppresses angiogenesis of cancer cells by reducing the expression of HIF-1 target genes, reduces glucose uptake, thereby sensitizing cells to growth under low glucose conditions, and decreases the extracellular acidification rate (ECAR) and oxygen consumption rate of cancer cells. Therefore, IDF-11774 reduces cancer cell growth through the regulation of cancer glycolytic metabolism and energy production.In vivoIDF-11774 exhibited substantial anticancer efficacy in mouse models containing KRAS, PTEN, or VHL mutations, which often occur in malignant cancers.Cell Research(from reference)Cell lines:HCT116 cells Concentrations:5, 10, 20 μM Incubation Time:18 h |
| 靶点: |
IC50: 3.65 μM (HIF-1α) |
| 体内研究: |
与对照组相比,口服 IDF-11774 处理的小鼠肿瘤中荧光素酶活性和 HIF-1α 积累受到强烈抑制。当每天口服 IDF-11774 持续两周时,在小鼠模型中观察到显著的剂量依赖性肿瘤消退。 |
| 参考文献: |
1. Ban HS, et al. The novel hypoxia-inducible factor-1α inhibitor IDF-11774 regulates cancer metabolism, thereby suppressing tumor growth. Cell Death Dis. 2017 Jun 1;8(6):e2843. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.714 ml |
13.568 ml |
27.136 ml |
| 5 mM |
0.543 ml |
2.714 ml |
5.427 ml |
| 10 mM |
0.271 ml |
1.357 ml |
2.714 ml |
| 50 mM |
0.054 ml |
0.271 ml |
0.543 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。 |