生物活性 靶点 体外研究 体内研究
ChemicalBook  CAS数据库列表  220619-73-8

220619-73-8

220619-73-8,220619-73-8,结构式
220619-73-8
  • CAS号:220619-73-8
  • 英文名:VTP 194204
  • 中文名:220619-73-8
  • CBNumber:CB52667435
  • 分子式:C24H32O2
  • 分子量:352.51
  • MOL File:220619-73-8.mol
220619-73-8化学性质
  • 储存条件 :Store at -20°C
  • 溶解度 :Soluble in DMSO
  • 形态 :Solid
  • 颜色 :White to off-white

220619-73-8性质、用途与生产工艺

  • 生物活性 AGN194204 (IRX4204) 是一种具有口服活性的,选择性 RXR 激动剂,对 RXRα,RXRβ 和 RXRγ 的 Kd 值分别为 0.4 nM,3.6 nM 和 3.8 nM,EC50 分别为 0.2 nM,0.8 nM 和 0.08 nM。AGN194204 对 RAR 无活性,并具有抗炎和抗癌作用。
  • 靶点

    RXRα

    0.4 nM (Kd)

    RXRβ

    3.6 nM (Kd)

    RXRγ

    3.8 nM (Kd)

    RXRα

    0.2 nM (EC 50 )

    RXRβ

    0.8 nM (EC 50 )

    RXRγ

    0.08 nM (EC 50 )

  • 体外研究

    AGN194204 (NRX194204; 0-100 nM; 24 hours; E, RAW cells) treatment blocks the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells.
    AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells.

    Apoptosis Analysis

    Cell Line: SK-BR-3 human breast cancer cells
    Concentration: 1 μM
    Incubation Time: 72 hours
    Result: Induced apoptosis in lung and breast cancer cells.

    Western Blot Analysis

    Cell Line: E, RAW cells
    Concentration: 0 nM, 1 nM, 10 nM and 100 nM
    Incubation Time: 24 hours
    Result: Blocked the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells.
  • 体内研究

    AGN194204 (NRX194204; 30-60 mg/kg; oral administration; daily; for 15 weeks; female A/J mice) treatment significantly reduces the number and size of tumors on the surface of the lungs and reduces the total tumor volume per slide by 64% to 81% compared with the control group.

    Animal Model: Female A/J mice with vinyl carbamate
    Dosage: 30 mg/kg, 60 mg/kg
    Administration: Oral administration; daily; for 15 weeks
    Result: Significantly reduced the number and size of tumors on the surface of the lungs and reduced the total tumor volume per slide by 64% to 81% compared with the control group.
220619-73-8上下游产品信息
上游原料
下游产品
220619-73-8生产厂家
  • 公司名称:TargetMol Chemicals Inc.
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