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ChemicalBook  CAS数据库列表  5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione

5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione

生物活性 靶点 体外研究 体内研究
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione,667880-38-8,结构式
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
  • CAS号:667880-38-8
  • 英文名:5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
  • 中文名:5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
  • CBNumber:CB32060973
  • 分子式:C24H23N3O3S
  • 分子量:433.52
  • MOL File:667880-38-8.mol
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione化学性质
  • 密度 :1.30±0.1 g/cm3(Predicted)
  • 储存条件 :Store at -20°C
  • 溶解度 :62.5 mg/mL in DMSO
  • 酸度系数(pKa) :5.34±0.20(Predicted)
  • 形态 :Solid
  • 颜色 :Yellow to orange

5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione性质、用途与生产工艺

  • 生物活性 ZLDI-8 是一种 Notch 活化/裂解酶 ADAM-17 抑制剂，可抑制 Notch 蛋白的裂解，并降低促存活/抗凋亡和上皮-间质转化相关蛋白的表达。ZLDI-8 还是一种竞争性和不可逆的酪氨酸磷酸酶 (Lyp) 抑制剂，IC50 为 31.6 μM，Ki 为 26.22 μM。ZLDI-8 以 IC50 为 5.32 μM 抑制 MHCC97-H 细胞的生长。
  • 靶点

    ADAM-17
    IC50: 31.6 μM (Tyrosine phosphatase)
    Ki: 26.22 μM (Tyrosine phosphatase)

  • 体外研究

    ZLDI-8 (0.03-30 μM; 6-72 hours; MHCC97-H cells) treatment reduces cell viability in a time- and dose-dependent manner.
    ZLDI-8 (1-10 μM; 6-72 hours; MHCC97-H cells) significantly decreases the level of NICD and the accumulation of NICD in the nucleus. ZLDI-8 could also reduce the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2. And also increases the expression of epithelial marker E-Cadherin and reduced mesenchymal markers N-Cadherin and Vimentin.
    ZLDI-8 enhances chemotherapy effects on tumor cell proliferation blockage, induction of apoptosis and cell-cycle arrest by inhibiting Notch pathway and blocking chemical resistance.

    Cell Viability Assay

    Cell Line: MHCC97-H cells
    Concentration: 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
    Incubation Time: 6 hours, 12 hours, 24 hours, 48 hours, 72 hours
    Result: Emerged cytotoxic effect on MHCC97-H cells in a time- and dose-dependent manner.

    Western Blot Analysis

    Cell Line: MHCC97-H cells
    Concentration: 1 μM, 3 μM, 10 μM
    Incubation Time: 6 hours, 12 hours, 24 hours, 48 hours, 72 hours
    Result: Significantly decreased the level of NICD and the accumulation of NICD in the nucleus. Also reduced the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2
  • 体内研究

    ZLDI-8 (0.2-2 mg/kg; intraperitoneal injection; every two days; for 20 days; nude mice) treatment enhances the effect of Sorafenib on inhibiting tumor growth in nude HCC-bearing mice model.

    Animal Model: Nude mice with MHCC-97H cells
    Dosage: 2 mg/kg, 1 mg/kg, 500 μg/kg, or 200 μg/kg
    Administration: Intraperitoneal injection; every two days; for 20 days
    Result: Inhibited tumor growth in nude HCC-bearing mice model.
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5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione生产厂家
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