生物活性 靶点 体外研究 体内研究 CGP 52411 试剂级价格
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CGP 52411

CGP 52411,145915-58-8,结构式
CGP 52411
  • CAS号:145915-58-8
  • 英文名:DAPH
  • 中文名:CGP 52411
  • CBNumber:CB2498023
  • 分子式:C20H15N3O2
  • 分子量:329.35
  • MOL File:145915-58-8.mol
CGP 52411化学性质
  • 熔点 :199-202℃
  • 密度 :1.374
  • 储存条件 :2-8°C
  • 溶解度 :DMSO: ~30 mg/mL
  • 酸度系数(pKa) :9.06±0.20(Predicted)
  • 形态 :solid
  • 颜色 :orange
安全信息
  • 安全说明 :36/37
  • WGK Germany :3

CGP 52411性质、用途与生产工艺

  • 生物活性 CGP52411 (DAPH) 是一种高选择性,有效,口服活性和 ATP 竞争性的 EGFR 抑制剂,IC50 为 0.3 μM。CGP52411 阻止有毒的 Ca2+ 离子流入神经元细胞,并显着抑制和逆转与阿尔茨海默症相关的 β-amyloid (Aβ42) 原纤维聚集物的形成。
  • 靶点

    EGFR

    0.3 μM (IC 50 )

    Amyloid-β

  • 体外研究

    CGP52411 (DAPH; 0-100 μM; 90 minutes; A431 cells) treatment inhibits autophosphorylation and c-src autophosphorylation in vitro in a dose-dependent manner with IC 50 s of 1 μM and 16 μM, respectively. CGP52411 treatment also shows a concentration-dependent reduction in tyrosine phosphorylation of p185c-erbB2 with an IC 50 value of 10 μM.
    CGP52411 (DAPH) inhibits c-src kinase with an IC 50 value of 16 μM. CGP52411 inhibits PKC isozymes isolated from porcine brain with an IC 50 of 80 μM. CGP52411 inhibits conventional PKC isozymes (cPKCs α, β-1, β-2, and γ) but not nonconventional PKC isozymes (nPKCs δ, ε, and ζ) or atypical PKC isozymes (aPKC η).

    Western Blot Analysis

    Cell Line: A431 cells
    Concentration: 0 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
    Incubation Time: 90 minutes
    Result: Inhibited autophosphorylation in vitro in a dose-dependent manner with an IC 50 of 1 μM. c-src autophosphorylation was inhibited with an IC 50 of 16 μM. And also resulted in a concentration-dependent reduction in tyrosine phosphorylation of p 185c-erbB2 , with an estimated IC 50 value of 10 μM.
  • 体内研究

    CGP52411 (3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg; oral administration; daily; for 15 days; female BALB/c nude mice) treatment in vivo against xenografts of the A431 and SK-OV-3 tumors, and has antitumor activity.

    Animal Model: Female BALB/c nude mice injected with A431cells
    Dosage: 3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg
    Administration: Oral administration; daily; for 15 days
    Result: Antitumor efficacy was obtained at doses between 50 mg/kg and 6.3 mg/kg.
CGP 52411上下游产品信息
上游原料
下游产品
CGP 52411 试剂级价格
  • 更新日期:2021/03/30
  • 产品编号:S0745
  • 产品名称:CGP 52411 CGP52411
  • CAS编号:145915-58-8
  • 包装:2mg
  • 价格:3906.63元
CGP 52411生产厂家
  • 公司名称:SIGMA
  • 联系电话:--
  • 电子邮件:
  • 国家:瑞士
  • 产品数:6896
  • 优势度:91
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