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ChemicalBook  CAS数据库列表  5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮

5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮

生物活性 靶点 体外研究 体内研究
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮,327033-36-3,结构式
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
  • CAS号:327033-36-3
  • 英文名:SMI-4a
  • 中文名:5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
  • CBNumber:CB12650480
  • 分子式:C11H6F3NO2S
  • 分子量:273.23
  • MOL File:327033-36-3.mol
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮化学性质
  • 熔点 :181-183℃ (methanol )
  • 密度 :1.530±0.06 g/cm3(Predicted)
  • 储存条件 :2-8°C
  • 溶解度 :≥ 9.4mg/mL in DMSO
  • 形态 :White to off-white solid.
  • 酸度系数(pKa) :7.26±0.20(Predicted)
安全信息

5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮性质、用途与生产工艺

  • 生物活性 TCS-PIM-1-4a (SMI-4a) 是一种泛-Pim 激酶抑制剂，可通过激活 AMPK 来阻断 mTORC1 的活性。TCS-PIM-1-4a 可杀死多种髓样和淋巴样细胞系 (IC50 值为 0.8 μM 至 40 μM)。
  • 靶点

    Pim

  • 体外研究

    TCS-PIM-1-4a (10 μM; 24-48 hours; 6812/2 cells and Jurkat cells) treatment increases the population of cells in the G1 phase from 44.3% to 68.4% and from 56.2% to 67.1% in 6812/2 and Jurkat, respectively. S-phase cells are decreased in 6812/2, whereas only small changes are seen in Jurkat cells consistent with the lesser G1 block.
    TCS-PIM-1-4a (5 μM; 6 hours; 6812/2 cells and Jurkat cells) induces cell death by the induction of apoptosis.
    TCS-PIM-1-4a (5 μM; 4-8 hours; 6812/2 cells and Jurkat cells) prevents the increase in 4E-BP1 protein levels and inhibits mTOR-directed phosphorylation on Thr37/46.

    Cell Cycle Analysis

    Cell Line: 6812/2 cells and Jurkat cells
    Concentration: 10 μM
    Incubation Time: 24 hours, 48 hours
    Result: Induced cell-cycle arrest.

    Apoptosis Analysis

    Cell Line: 6812/2 cells and Jurkat cells
    Concentration: 5 μM
    Incubation Time: 6 hours
    Result: Led to an increase in the number of the cells positive for annexin V and negative for PI from 8.25% in the control to 21.85%.

    Western Blot Analysis

    Cell Line: 6812/2 cells and Jurkat cells
    Concentration: 10 μM
    Incubation Time: 4 hours, 8 hours
    Result: Prevented the increase in 4E-BP1 protein levels and inhibited mTOR-directed phosphorylation on Thr37/46.
  • 体内研究

    TCS-PIM-1-4a (SMI-4a; 60 mg/kg; oral gavage; twice daily; for 21 days; nu/nu nude mice) treatment causes a significant delay in the tumor growth without any change in the weight, blood counts, or chemistries.

    Animal Model: 18 Nu/nu nude mice with 6812/2 murine pre–T-LBL cells
    Dosage: 60 mg/kg
    Administration: Oral gavage; twice daily; for 21 days
    Result: Caused a significant delay in the tumor growth.
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