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ChemicalBook  CAS数据库列表  2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺

2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺

生物活性 靶点 体外研究 体内研究
2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺,732983-37-8,结构式
2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺
  • CAS号:732983-37-8
  • 英文名:BAY 61-3606
  • 中文名:2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺
  • CBNumber:CB1497948
  • 分子式:C20H18N6O3
  • 分子量:390.4
  • MOL File:732983-37-8.mol
2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺化学性质
  • 密度 :1.41
  • 储存条件 :2-8°C
  • 溶解度 :H2O: soluble
  • 形态 :solid
  • 颜色 :yellow
安全信息
  • WGK Germany :3

2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺性质、用途与生产工艺

  • 生物活性 BAY 61-3606 是一种有效的，具有口服活性的，ATP 竞争性的，可逆的选择性 Syk 抑制剂，Ki 为 7.5 nM，IC50 为 10 nM。BAY 61-3606 降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化。BAY 61-3606 降低 K-rn 细胞裂解物中 Syk 磷酸化。Bay 61-3606 作用于乳腺癌细胞，通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。
  • 靶点

    Ki: 7.5 nM (Syk)
    IC50: 10 nM (Syk)

  • 体外研究

    BAY 61-3606 (0.01-10 μM ; 48 hours) significantly reduces the cell viability of SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells in a dose-dependent matter. SH-SY5Y cells expressing high SYK levels are significantly more sensitive to BAY 61-3606 in comparison to SK-N-BEcells expressing very low or no SYK.
    BAY 61-3606 (0.4 and 0.8 μM; 4 or 24 hours) inhibits SYK activity by reducing ERK1/2 and Akt phosphorylation in neuroblastoma cell SH-SY5Y.
    BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation in K-rn cell lysates.

    Cell Viability Assay

    Cell Line: SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells
    Concentration: 0.01, 0.1, 1, and 10 μM
    Incubation Time: 48 hours
    Result: Significantly reduced the cell viability of both cell lines in a dose-dependent matter.

    Western Blot Analysis

    Cell Line: SH-SY5Y cells
    Concentration: 0.4 and 0.8 μM
    Incubation Time: 4 or 24 hours
    Result: Reduced the phosphorylation of ERK1/2 and Akt after a 4 or 24 h treatment.

    Western Blot Analysis

    Cell Line: K-rn cell lysates
    Concentration: 2 μM
    Incubation Time: 2 hours
    Result: Induced a large decrease of Syk phosphorylation.
  • 体内研究

    Bay 61-3606 (50 mg/kg; administered twice a week for two weeks by intraperitoneal injection) alone leads to more efficacious reductions than that of TNF-related apoptosis-inducing ligand (TRAIL; 10 mg/kg) alone in MCF-7 tumor xenograft-bearing BALB/c nude mice. Bay 61-3606 administered in TRAIL combination significantly reduces the volume of the xenografted tumor.

    Animal Model: Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft
    Dosage: 50 mg/kg
    Administration: Injected intraperitoneally twice a week with Bay 61-3606 (50 mg/kg), TRAIL (10 mg/kg) or a combination of Bay 61-3606 (50 mg/kg) and TRAIL (10 mg/kg); TRAIL was given 2 h after the injection of Bay 61-3606; for two weeks
    Result: Led to efficacious reductions in tumor growth.
2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺上下游产品信息
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2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺生产厂家
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