CC214-1

• 常用名: CC214-1
• 英文名: CC214-1
• CAS号: 1021920-32-0
• 分子量: 391.43
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₂₁N₇O₂
• 熔点: N/A
• 闪点: N/A

CC214-1用途

CC214-1是一种潜在有效的mTOR抑制剂,可诱导自噬[1],IC50为0.002μM。CC214-1被证明可用作mTOR激酶生物学探索的体外工具化合物。CC214-1可用于胶质母细胞瘤的研究[2]。

CC214-1名称

• 英文名: CC214-1

CC214-1生物活性

• 描述: CC214-1是一种潜在有效的mTOR抑制剂,可诱导自噬[1],IC50为0.002μM。CC214-1被证明可用作mTOR激酶生物学探索的体外工具化合物。CC214-1可用于胶质母细胞瘤的研究[2]。
• 相关类别:
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> mTOR
  研究领域 >> 癌症
• 靶点实验:

  mTOR:0.002 μM (IC50)

• 体外研究: CC214-1(0、0.1、1、2、5、10μM,8小时；2μM,24小时)与 雷帕霉素(HY-10219)协同作用,抑制 mTORC1信号传导和肿瘤细胞增殖[1] CC214-1(2μM,24小时)介导因 EGFRvIII表达和 PTEN缺失而导致胶质母细胞瘤细胞生长停滞的敏感性[1] CC214-1(5μM,0-48小时)将 LC3B-I大量脂化为 LC3B-II亚型,并诱导 GBM39细胞自噬[1] CC214-1对 mTOR的 IC50为 0.002μM[2]CC214-1(0-10μM,4天)可有效抑制 T细胞活化和 T细胞活化标记物的表达[3] 蛋白质印迹分析[1]细胞系：胶质母细胞瘤浓度：0,0.1,1,2,5,10μM；2μM培养时间：8h；24小时结果：在所有测试的胶质母细胞瘤细胞系中抑制mTORC1信号传导,有效抑制雷帕霉素抗性4E-BP1和mTORC2信号传导。抑制表达EGFRvIII的胶质母细胞瘤细胞中mTORC1依赖性4E-BP1和S6磷酸化,以及阻断过表达野生型EGFR的胶质母瘤细胞。免疫荧光[1]细胞系：胶质母细胞瘤浓度：2μM,5μM孵育时间：4h；0,4,12,24,48小时结果：诱导LC3B-II亚型的瞬时表达和Atg12与Atg5的结合,表明U87EGFRvIII细胞系中自噬流量的刺激。在GBM39细胞中将LC3B-I大量脂化为LC3B-II亚型并诱导自噬。细胞周期分析[3]细胞系：胶质母细胞瘤浓度：0-10μM培养时间：4天结果：在CD4+和CD8+T细胞亚群中诱导TEE细胞。
• 参考文献:

  [1]. Gini B, et al. The mTOR kinase inhibitors, CC214-1 and CC214-2, preferentially block the growth of EGFRvIII-activated glioblastomas. Clin Cancer Res. 2013 Oct 15;19(20):5722-32.

  [2]. Mortensen DS, et al. Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1588-91.

  [3]. Herrero-Sánchez MC, et al. Effect of mTORC1/mTORC2 inhibition on T cell function: potential role in graft-versus-host disease control. Br J Haematol. 2016 Jun;173(5):754-68.

CC214-1物理化学性质

• 分子式: C₂₀H₂₁N₇O₂
• 分子量: 391.43

CC214-1靶点实验

查看更多实验

实验名称：Inhibition of ARK5 (unknown origin) assessed as remaining activity at 10 uM relative ... 来源：ChEMBL 靶标：NUAK family SNF1-like kinase 1 External Id：CHEMBL2352549

实验名称：Inhibition of IKBKE (unknown origin) assessed as remaining activity at 10 uM relative... 来源：ChEMBL 靶标：Inhibitor of nuclear factor kappa-B kinase subunit epsilon External Id：CHEMBL2352553

实验名称：Inhibition of HIPK3 (unknown origin) assessed as remaining activity at 10 uM relative... 来源：ChEMBL 靶标：Homeodomain-interacting protein kinase 3 External Id：CHEMBL2352552

实验名称：Inhibition of HIPK2 (unknown origin) assessed as remaining activity at 10 uM relative... 来源：ChEMBL 靶标：Homeodomain-interacting protein kinase 2 External Id：CHEMBL2352551

实验名称：Inhibition of GSG2 (unknown origin) assessed as remaining activity at 10 uM relative ... 来源：ChEMBL 靶标：Serine/threonine-protein kinase haspin External Id：CHEMBL2352550

实验名称：Inhibition of PAK1 (unknown origin) assessed as remaining activity at 10 uM relative ... 来源：ChEMBL 靶标：Serine/threonine-protein kinase PAK 1 External Id：CHEMBL2352802

实验名称：Inhibition of MNK1 (unknown origin) assessed as remaining activity at 10 uM relative ... 来源：ChEMBL 靶标：MAP kinase-interacting serine/threonine-protein kinase 1 External Id：CHEMBL2352801

实验名称：Inhibition of LRRK2 G2019S mutant (unknown origin) assessed as remaining activity at ... 来源：ChEMBL 靶标：Leucine-rich repeat serine/threonine-protein kinase 2 External Id：CHEMBL2352800

实验名称：Inhibition of IRK1 (unknown origin) assessed as remaining activity at 10 uM relative ... 来源：ChEMBL 靶标：Inward rectifier potassium channel 2 External Id：CHEMBL2352554

实验名称：Inhibition of Txk (unknown origin) assessed as remaining activity at 10 uM relative t... 来源：ChEMBL 靶标：Tyrosine-protein kinase TXK External Id：CHEMBL2352804

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