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NSC139021

CAS No. 1147-56-4

NSC139021 ( ERGi-USU )

产品货号. M20631 CAS No. 1147-56-4

NSC139021 是一种 Rio2 激酶 (RIOK2) 抑制剂,可抑制 ERG 蛋白。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
100MG ¥332 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    NSC139021
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    NSC139021 是一种 Rio2 激酶 (RIOK2) 抑制剂,可抑制 ERG 蛋白。
  • 产品描述
    NSC139021 is a Rio2 kinase (RIOK2) inhibitor that inhibits ERG protein.
  • 体外实验
    NSC139021 selectively inhibits growth of ERGpositive cancer cell lines with minimal effect on normal prostate or endothelial cells or ERG-negative tumor cell lines. The IC50 of NSC139021 for cell growth inhibition of responsive cell lines range between 30 nM to 400 nM. Combination of NSC139021 with enzalutamide shows additive effects in inhibiting growth of VCaP cells. A screen of kinases reveal that NSC139021 directly bound the ribosomal biogenesis regulator atypical kinase RIOK2 and induces ribosomal stress signature.
  • 体内实验
    NSC139021 treatment inhibits growth of ERG-positive VCaP tumor xenografts with no apparent toxicity. Significant (P<0.05, P<0.005) inhibition of tumor growth is noted at day 26 in treatment groups indicating 44% (100 mg/kg) and 65% (150 mg/kg) reduction of tumor burden. At 100 mg/kg and 150 mg/kg, no apparent toxicity including weight loss, lethargy, diarrhea, loss of appetite, respiratory distress, or overall drug related toxicity is observed. .
  • 同义词
    ERGi-USU
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    Rio2 kinase (RIOK2)
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    1147-56-4
  • 分子量
    255.3
  • 分子式
    C13H9N3OS
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO:62 mg/mL (242.85 mM)
  • SMILES
    Oc1ccc2ccccc2c1N=Nc1nccs1
  • 化学全称
    1-[2-(2-Thiazolyl)diazenyl]-2-naphthalenol

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1.Mohamed A A Xavier C P Sukumar G et al. Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth[J]. Cancer Research 2018:canres.2949.2017.
产品手册
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