| 产品描述: | KLF抑制剂;KLF Inhibitors;;InformationML264 ML264 (CID-51003603), a selectively inhibitor of kruppel-like factor 5 (KLF5) ,potently Inhibits Growth of Colorectal Cancer.TargetsKLF5 (Cell-based assay for proliferation of DLD-1 cells) 29 nMIn vitroML264 potently halts DLD-1 viability (IC50 = 29 nM) with high maximal effect (>90%). DLD-1 cells are human colorectal adenocarcinoma cells. ML264 has significant effects at submicromolar doses on other cell types as well, including HCT116 (human colorectal carcinoma), HT29 (human colorectal adenocarcinoma), and SW620 (human colorectal adenocarcinoma). The IEC-6 anti-target (a nontransformed rat intestinal epithelial cell line) is largely unaffected, with inhibition below 50% at the highest dose.This compound potently inhibits proliferation of CRC cells in vitro through modifications of the cell cycle profile.In vivoIn an established xenograft mouse model of colon cancer, ML264 efficiently inhibits growth of the tumor within five days of treatment. this effect is caused by a significant reduction in proliferation and that ML264 potently inhibits the expression of KLF5 and EGR1, a transcriptional activator of KLF5.Cell Research(from reference)Cell lines:DLD-1 and HCT116 colorectal cancer cell lines Concentrations:10μM Incubation Time:24, 48, 72h |
| 靶点: |
KLF5 |
| 体内研究: |
每天单次注射 10 mg/kg 的 ML264 不会显著影响肿瘤生长。然而,每天两次以 10 mg/kg 或 25 mg/kg 的剂量注射 ML264 会导致肿瘤生长显著减少,并且这种效果最早可在第一次注射后两天检测到。数据还显示 ML264 对肿瘤体积有浓度依赖性影响。肿瘤生长的统计分析显示,与在第 5 天和第 10 天仅接受载体的小鼠相比,每天两次接受 ML264 处理的小鼠的肿瘤大小显著减小。 |
| 参考文献: |
1. Bialkowska A, et al. ML264: An Antitumor Agent that Potently and Selectively Inhibits Krüppel-like Factor Five (KLF5) Expression: A Probe for Studying Colon Cancer Development and Progression. 2. Ruiz de Sabando A, et al. ML264, A Novel Small-Molecule Compound That Potently Inhibits Growth of Colorectal Cancer. Mol Cancer Ther. 2016 Jan;15(1):72-83. |
| 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 |
2.598 ml |
12.991 ml |
25.982 ml |
| 5 mM |
0.52 ml |
2.598 ml |
5.196 ml |
| 10 mM |
0.26 ml |
1.299 ml |
2.598 ml |
| 50 mM |
0.052 ml |
0.26 ml |
0.52 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。 |