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ML-264

CAS No. 1550008-55-3

ML-264 ( ML264 | ML 264 )

产品货号. M12198 CAS No. 1550008-55-3

一种有效的、选择性的 KLF5 表达抑制剂,对与 KLF5 通路相关的激酶没有影响。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥543 有现货
10MG ¥826 有现货
25MG ¥1685 有现货
50MG ¥2940 有现货
100MG ¥4431 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    ML-264
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    一种有效的、选择性的 KLF5 表达抑制剂,对与 KLF5 通路相关的激酶没有影响。
  • 产品描述
    A potent, selective of KLF5 expression inhibtor, withour effect on kinases associated with the KLF5 pathway; inhibits the proliferation of DLD-1 cells with IC50 of 29 nM, and several other KLF5-expressing cell types as well HCT116, IC50 560 nM; HT29, IC50=130 nM; SW620, IC50=430 nM); potently inhibits proliferation of colorectal cancer cells in vitro through modifications of the cell-cycle profile; efficiently inhibits growth of the tumo in an established xenograft mouse model of colon cancer.Colon Cancer Preclinical(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.
  • 体外实验
    ——
  • 体内实验
    ——
  • 同义词
    ML264 | ML 264
  • 通路
    Nuclear Receptor/Transcription Factor
  • 靶点
    KLF
  • 受体
    KLF5
  • 研究领域
    Cancer
  • 适应症
    Colon Cancer

化学信息

  • CAS Number
    1550008-55-3
  • 分子量
    384.8777
  • 分子式
    C17H21ClN2O4S
  • 纯度
    >98% (HPLC)
  • 溶解度
    10 mM in DMSO
  • SMILES
    O=C(NCC(N(C(CC1)CCS1(=O)=O)C)=O)/C=C/C2=CC=CC(Cl)=C2
  • 化学全称
    2-Propenamide,3-(3-chlorophenyl)-N-[2-[methyl(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]-2-oxoethyl]-,(2E)-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Bialkowska A, et al. Probe Reports from the NIH Molecular Libraries Program [Internet]. 2. Ruiz de Sabando A, et al. Mol Cancer Ther. 2016 Jan;15(1):72-83.
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    一种有效的、选择性的 KLF5 表达抑制剂,对与 KLF5 通路相关的激酶没有影响。