生物活性 靶点 体外研究 体内研究 1227637-23-1 试剂级价格
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ChemicalBook  CAS数据库列表  1227637-23-1

1227637-23-1

生物活性 靶点 体外研究 体内研究 1227637-23-1 试剂级价格
1227637-23-1,1227637-23-1,结构式
1227637-23-1
  • CAS号:1227637-23-1
  • 英文名:BC2059
  • 中文名:1227637-23-1
  • CBNumber:CB03038499
  • 分子式:C28H36N4O6S2
  • 分子量:588.74
  • MOL File:1227637-23-1.mol
1227637-23-1化学性质
  • 沸点 :757.6±70.0 °C(Predicted)
  • 密度 :1.46±0.1 g/cm3(Predicted)
  • 储存条件 :under inert gas (nitrogen or Argon) at 2-8°C
  • 溶解度 :DMSO: 125 mg/mL (212.32 mM)
  • 酸度系数(pKa) :10.07±0.20(Predicted)
  • 形态 :Solid
  • 颜色 :White to light yellow

1227637-23-1性质、用途与生产工艺

  • 生物活性 Tegatrabetan (BC2059) 是一种 β-Catenin 的拮抗剂。Tegatrabetan (BC2059) 会破坏β-catenin与scaffold protein transducin β-like 1 (TBL1)的结合以及蛋白酶体降解并降低β-catenin核水平。
  • 靶点
    TargetValue
    β-catenin
    ()
  • 体外研究

    Tegatrabetan (BC2059; 20-100 nM; 48 hours) inhibits cell proliferation in suspension culture over 120 hours and induces apoptosis of cultured human acute myeloid leukemia (AML) HL-60, OCI-AML3 and MV4-11 cells dose-dependently.
    Tegatrabetan (20 and 50 nM; 24 hours) induces a modest but significant accumulation of cells in the G0/G1 phase, with a concomitant decline in the G2/M phase of the cell cycle.
    Tegatrabetan (100 nM, 24 hours) depletes the levels of β-catenin and its target genes, including c-MYC and survivin without affecting the levels of the TBL1 in OCI-AML3, HL-60 and MV4-11 cells.

    Cell Proliferation Assay

    Cell Line: HL-60, OCI-AML3 and MV4-11 cells
    Concentration: 20, 50, and 100 nM
    Incubation Time: 48 hours
    Result: Dose-dependently inhibited cell proliferation.

    Cell Cycle Analysis

    Cell Line: OCI-AML3 cells
    Concentration: 20 and 50 nM
    Incubation Time: 24 hours
    Result: Dose-dependently induced cell cycle growth arrest.

    Western Blot Analysis

    Cell Line: OCI-AML3, HL-60 and MV4-11 cells
    Concentration: 100 nM
    Incubation Time: 24 hours
    Result: Treatment depleted β-Catenin expression levels.
  • 体内研究

    Tegatrabetan (BC2059; 1.0 or 5.0 mg/kg/day; intravenously) significantly improves the median survival of the mice from approximately 17.5 to 39 days. Treatment with Tegatrabetan (10 mg/kg/day; intravenously) alone further improves the median survival to 51.5 days.

    Animal Model: NOD/SCID mice bearing OCI-AML3 xenografts
    Dosage: 1 mg/kg; 5 mg/kg; 10 mg/kg
    Administration: Intravenously; 1 mg/kg daily 4 days per week or 5 mg/kg or 10 mg/kg of BC2059 twice per week (Tuesday and Thursday) for 3 weeks.
    Result: Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts.
1227637-23-1上下游产品信息
上游原料
下游产品
1227637-23-1 试剂级价格
  • 更新日期：2024/04/30
  • 产品编号：S0733
  • 产品名称：1227637-23-1 Tegatrabetan (BC-2059)
  • CAS编号：1227637-23-1
  • 包装：5mg
  • 价格：2269.4元
  • 更新日期：2024/04/30
  • 产品编号：S0733
  • 产品名称：Tegatrabetan (BC-2059)
  • CAS编号：1227637-23-1
  • 包装：10mM (1mL in DMSO)
  • 价格：2694.51元
1227637-23-1生产厂家
  • 公司名称：HANGZHOU CLAP TECHNOLOGY CO.,LTD
  • 联系电话：86-571-88216897,88216896 13588875226
  • 电子邮件：sales@hzclap.com
  • 国家：中国
  • 产品数：6313
  • 优势度：58
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