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ChemicalBook  CAS数据库列表  1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑

1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑

生物活性 靶点 体外研究 体内研究
1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑,162054-19-5,结构式
1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑
  • CAS号:162054-19-5
  • 英文名:1-[(4-METHYLSULFONYL)PHENYL]-3-TRIFLUOROMETHYL-5-(4-FLUOROPHENYL)PYRAZOLE
  • 中文名:1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑
  • CBNumber:CB6486473
  • 分子式:C17H12F4N2O2S
  • 分子量:384.35
  • MOL File:162054-19-5.mol
1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑化学性质
  • 储存条件 :Store at +4°C
  • 溶解度 :DMSO: ≥20mg/mL
  • 形态 :powder
  • 颜色 :white to off-white
安全信息
  • 危险品标志 :T
  • 危险类别码 :25
  • 安全说明 :45-24/25-22
  • WGK Germany :3

1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑性质、用途与生产工艺

  • 生物活性 SC-58125 是一种有效的和选择性的环氧合酶 2 (COX-2) 的抑制剂，IC50 值为 0.04 μM。SC-58125 在体外和体内均表现出抗肿瘤活性，还可以抑制炎症部位的水肿并具有镇痛作用。
  • 靶点

    hCOX-2

    0.04 μM (IC 50 )

    hCOX-1

    >100 μM (IC 50 )

  • 体外研究

    SC-58125 (0.001-100 μM) has a high degree of selectivity for the inducible form of COX-2 (IC 50 =1 μM) over the COX-1 (IC 50 >100 μM).
    SC-58125 (10 μM; 20-140 s) is time-dependent and is complete by 1 min, with a half-maximal inhibition at 20 s.
    SC-58125 (25-100 μM; 3 d) inhibits the in vitro growth of HCA-7 and LLC cells.
    SC-58125 (100 µM; 12 h) induces G 2 arrest in LLC cells.
    SC-58125 (25-100 μM; 3 d) decreases p34 cdc2 levels in HCA-7 cells.
    SC-58125 (100 µM; 24 or 72 h) does not induce apoptosis of HCA-7 and LLC cells.

    Cell Proliferation Assay

    Cell Line: HCA-7 and LLC cells
    Concentration: 0, 25, 50, 100 μM
    Incubation Time: 3 days
    Result: Reduced the cell number and MTT activity in both cell lines in a dose-dependent manner.

    Cell Cycle Analysis

    Cell Line: LLC cells
    Concentration: 100 μM
    Incubation Time: 12 hours
    Result: Increased in the number of cells containing 4n DNA content in a dose- and time-dependent manner.
    Reduced the number of mitotic figures.

    Western Blot Analysis

    Cell Line: HCA-7 cells
    Concentration: 0, 25, 50, 100 μM
    Incubation Time: 3 days
    Result: Resulted in a dose-dependent decrease in p34 cdc2 activity with strong inhibition, even at the lowest concentration.
  • 体内研究

    SC-58125 (10 mg/kg; i.p. every 48 h) inhibits the growth of established colorectal cancer xenografts in mice.
    SC-58125 (10 mg/kg; a single i.p.) reduces tumor PGE2 levels in mice.
    SC-58125 (10 mg/kg; a single i.p.) does not change the tumor levels of COX-1 and COX-2 protein in mice.

    Animal Model: Athymic Sprague-Dawley mice are injected HCA-7 cells
    Dosage: 10 mg/kg
    Administration: I.p. every 48 h; at the time of tumor implantation or 2 and 4 weeks later
    Result: Decreased the tumor growth rates significantly.
1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑上下游产品信息
上游原料
下游产品
1-[(4-甲基磺酰基)苯基]-3-三氟甲基-5-(4-氟苯基)吡唑生产厂家
  • 公司名称：北京百灵威科技有限公司
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  • 联系电话：400-400-400-9004166 18616739031
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  • 国家：美国
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