MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

ML264

CAS No. : 1550008-55-3

MCE 站：ML264

产品活性：ML264 是一种抗肿瘤剂，可有效和选择性地抑制 Krüppel 样因子 5 (KLF5) 表达。

研究领域：MAPK/ERK Pathway

作用靶点：KLF

In Vitro: ML264 is highly active (IC₅₀=29 nM is a cell-based assay for proliferation of DLD-1 cells, IC₅₀=81 nM in a cell-based luciferase assay). ML264 lacks cytotoxicity in the IEC-6 control cell line (IC₅₀>50 μM, <50% inhibition is observed at 100 μM). Robust activity is also seen in several other KLF5-expressing cell types as well (e.g., HCT116, IC₅₀=560 nM; HT29, IC₅₀=130 nM; SW620, IC₅₀=430 nM). Western blot analysis shows that ML264 significantly reduces KLF5 expression. The effects of ML264 are tested on the rate of cell proliferation of colon cancer cells lines DLD-1 and HCT116 over 72 hours. ML264 efficiently inhibits the rate of proliferation of both cell lines. A significant decrease in proliferation is evident within 24 hours of treatment and by 72 hours the live cell numbers of ML264-treated and vehicle-treated cells differed by 15- to 30- fold. An MTS assay that allows the quantification of metabolically active cells is performed. ML264 treatment significantly reduces the number of cells undergoing mitosis in DLD-1 cells at 24, 48 and 72 hours.

In Vivo: Single daily injections of ML264 at 10 mg/kg do not significantly affect tumor growth. However, twice daily injections of ML264 at 10 mg/kg or 25 mg/kg result in significant reductions in tumor growth, and this effect can be detected as early as two days after the first injection. The data also show that there is a concentration-dependent effect of ML264 on the tumor volume. Statistical analysis of tumor growth reveals significant tumor size reduction in mice treated twice daily with ML264 compared to those receiving only vehicle at day 5 and 10.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  MAPK Compound Library  |  Anti-Cancer Compound Library  |  Covalent Screening Library  |  Oxygen Sensing Compound Library  |  CID 5951923

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。