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Torin 2

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  • ¥295 - 8460
  • MedChemExpress(MCE)已认证
  • 美国
  • HY-13002
  • 2025年07月16日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.

    • 库存

      货期:1-2天

    • 供应商

      MedChemExpress LLC

    • CAS号

      1223001-51-1

    • 规格

      10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg/100 mg/200 mg

    规格:10 mM * 1 mL产品价格:¥720.0
    规格:1 mg产品价格:¥295.0
    规格:5 mg产品价格:¥650.0
    规格:10 mg产品价格:¥1100.0
    规格:50 mg产品价格:¥3300.0
    规格:100 mg产品价格:¥4900.0
    规格:200 mg产品价格:¥8460.0

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    Torin 2

    CAS No. : 1223001-51-1

    MCE 国际站:Torin 2

    产品活性:Torin 2 是一种 mTOR 抑制剂,抑制细胞内 mTOR 活性,EC50 为 0.25 nM,比作用于 PI3K (EC50: 200 nM) 选择性高 800 倍。体外酶实验中,Torin 2 还抑制 DNA-PKIC50 为 0.5 nM。Torin 2 抑制 mTORC1mTORC2

    研究领域:PI3K/Akt/mTOR  |  Cell Cycle/DNA Damage  |  Autophagy  |  Apoptosis

    作用靶点:mTOR  |  DNA-PK  |  Autophagy  |  Apoptosis

    In Vitro: Torin 2 is subject to further profiling against a panel of lipid kinases with IC50s of 2.81 nM, 0.5 nM, 5.67 nM, 8.58 nM, 18.3 nM, 24.5 nM and 28.1 nM for mTOR, DNA-pK, p110γ, hVPS34, PI4Kβ, PI3K-C2β and PI3K-C2α, respectively. Torin 2 (Torin2) possesses a 250 pM EC50 for inhibiting mTOR in cells while maintaining 800-fold cellular selectivity relative to inhibition of PI3K and most other protein kinases. Torin 2 (Torin2) exhibits potent biochemical and cellular activity against PIKK family kinases including ATM (EC50 28 nM), ATR (EC50 35 nM) and DNA-PK (EC50 118 nM). Torin 2 potently inhibits T308 of Akt, a direct substrate of PDK1 and an indirect substrate of PI3Ks, with an EC50 of less than 10 nM. Torin-2 can suppress both?mTORC1 and mTORC2.

    In Vivo: Torin 2 exhibits good bioavailability and exposure and can maintain strong inhibition of mTOR activity in lung and liver to at least six hours after a single dose of 20 mg/kg. Torin 2 is easier to produce on scale and exhibits improved pharmacokinetic properties which should enable it use in vivo experiments. Torin 2 strongly suppresses pS6K(T389) and p4EBP1(T37/46) and partly suppresses pAkt(T308). Treatment of mice with AZD6244 at 25 mg/kg results in a profound inhibition of pERK. Combined administration of Torin 2 (40 mg/kg) and AZD6244 (25 mg/kg) demonstrates strong inhibition of all pharmacodynamics markers. Treatment with Torin 2 and Rapamycin induces IL-6 secretion by astrocytes and may contribute to the reduction of mechanical hypersensitivity after SCI. Torin1 and Torin 2 treatment increases IL-6 mRNA, suggesting that the PI3K-mTOR pathway is a negative regulator of IL-6 expression in astrocytes. Importantly, Torin 2 treatment does not show any cell toxicity, as no signs of cell death are observed by TUNEL assay or by detection of cleaved-caspase 3 by western blotting.

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      所介导,为确定「铁死亡」的发生是通过何靶点所调控,研究者利用了可抑制 mTORC1 活性的雷帕霉素类似物 Temsirolimus(CCI-779)进行实验,发现 CCI-779 可以使癌细胞对「铁死亡」敏感。 由于 CCI-779 和 mTOR 催化抑制剂 Torin 都可以恢复癌细胞对「铁死亡」的敏感性,研究者假设 mTORC1 而不是 mTORC2,负责具有 PI3K-AKT 通路突变癌细胞的抗性。 研究发现,短发夹 RNA 介导的 RAPTOR(mTORC1 的组成部分)沉默使 MDA

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