2. PI3K/Akt/mTOR Cell Cycle/DNA Damage Autophagy Apoptosis
  3. mTOR DNA-PK Autophagy Apoptosis
  4. Torin 2

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-PK，IC50 为 0.5 nM。Torin 2 抑制 mTORC1 和 mTORC2。

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Torin 2 Chemical Structure

Torin 2 Chemical Structure

CAS No. : 1223001-51-1

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10 mM * 1 mL in DMSO ￥720
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Customer Review

Torin 2 相关抗体

Top Publications Citing Use of Products

    Torin 2 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Dec;17(12):2676-2688.  [Abstract]

    The mTORC1/2 inhibitor Torin2 suppresses protein synthesis in the EW8 and TC71 Ewing sarcoma cell lines.

    查看 mTOR 亚型特异性产品:

    查看所有亚型
    mTOR mTORC1 mTORC2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.

    IC50 & Target[1][4]

    mTOR

    2.81 nM (IC50)

    mTOR

    0.25 nM (EC50, Cell Assay)

    mTORC1

     

    mTORC2

     

    DNA-PK

    0.5 nM (IC50)

    p110γ

    5.67 nM (IC50)

    PI3K-C2β

    24.5 nM (IC50)

    PI3K-C2α

    28.1 nM (IC50)

    hVps34

    8.58 nM (IC50)

    PI3K

    200 nM (EC50, Cell Assay)

    ΡΙ4Κβ

    18.3 nM (IC50)

    Autophagy

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HCT-116 GI50
    32.19 nM
    Compound: Torin2
    Growth inhibition of human HCT116 cells measured after 72 hrs by Celltiter-Glo assay
    Growth inhibition of human HCT116 cells measured after 72 hrs by Celltiter-Glo assay
    		[PMID: 32911078]
    HeLa IC50
    < 10 nM
    Compound: 15
    Inhibition of N-terminally FLAG-tagged mTORC2 (unknown origin) expressed in human HeLa cells using S6K1 or Akt1 as substrate after 20 mins by immunoblotting assay
    Inhibition of N-terminally FLAG-tagged mTORC2 (unknown origin) expressed in human HeLa cells using S6K1 or Akt1 as substrate after 20 mins by immunoblotting assay
    		[PMID: 29211480]
    HeLa GI50
    97.95 nM
    Compound: Torin2
    Growth inhibition of human HeLa cells measured after 72 hrs by Celltiter-Glo assay
    Growth inhibition of human HeLa cells measured after 72 hrs by Celltiter-Glo assay
    		[PMID: 32911078]
    MOLM-13 IC50
    < 1 nM
    Compound: Torin2
    Antiproliferative activity against human MOLM13 cells by Cell-Titer Glo assay
    Antiproliferative activity against human MOLM13 cells by Cell-Titer Glo assay
    		[PMID: 30370766]
    MOLM-14 IC50
    < 1 nM
    Compound: Torin2
    Antiproliferative activity against human MOLM14 cells by Cell-Titer Glo assay
    Antiproliferative activity against human MOLM14 cells by Cell-Titer Glo assay
    		[PMID: 30370766]
    MV4-11 IC50
    < 1 nM
    Compound: Torin2
    Antiproliferative activity against human MV4-11 cells by Cell-Titer Glo assay
    Antiproliferative activity against human MV4-11 cells by Cell-Titer Glo assay
    		[PMID: 30370766]
    PC-3 EC50
    200 nM
    Compound: 3, Torin2
    Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting
    Inhibition of PI3Kalpha in human PC3 cells expressing Akt1 S473D mutant assessed as phosphorylation of Akt Thr308 by immunoblotting
    		[PMID: 21322566]
    RD CC50
    0.04 μM
    Compound: 1
    Cytotoxicity against human RD cells incubated for 4 days by CellTiter-Glo luminescence assay
    Cytotoxicity against human RD cells incubated for 4 days by CellTiter-Glo luminescence assay
    		[PMID: 31082764]
    体外研究
    (In Vitro)

    Torin 2 针对一组脂质激酶进行进一步分析，mTOR、DNA-分别为 pK、p110γ、hVPS34、PI4Kβ、PI3K-C2β 和 PI3K-C2α。Torin 2 (Torin2) 具有 250 pM EC50 用于抑制细胞中的 mTOR，同时相对于抑制 PI3K 和大多数其他蛋白激酶保持 800 倍的细胞选择性[1]。Torin 2 (Torin2) 对 PIKK 家族激酶表现出有效的生化和细胞活性，包括 ATM (EC50 28 nM)、ATR (EC50 35 nM) 和 DNA-PK (EC50 118 nM)。Torin 2 有效抑制 Akt 的 T308，Akt 是 PDK1 的直接底物和 PI3K 的间接底物，EC50 小于 10 nM[2]。Torin-2 可以同时抑制 mTORC1 和 mTORC2[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Torin 2 相关抗体:
    体内研究
    (In Vivo)

    Torin2 表现出良好的生物利用度和暴露，并且在单剂量 20 mg/kg 后可以维持对肺和肝脏中 mTOR 活性的强烈抑制至少 6 小时。Torin 2 更容易大规模生产，并表现出改进的药代动力学特性，这应该使其能够用于体内实验[1]。Torin 2 强烈抑制 pS6K (T389) 和 p4EBP1 (T37/46) 并部分抑制 pAkt (T308)。用 25 mg/kg 的 AZD6244 处理小鼠可显著抑制 pERK。Torin 2 (40 mg/kg) 和 AZD6244 (25 mg/kg) 的联合给药表现出对所有药效学标志物的强烈抑制[2]。用 Torin 2 和雷帕霉素处理可诱导星形胶质细胞分泌 IL-6，并可能有助于减少 SCI 后的机械超敏反应。Torin1 和 Torin 2 处理增加了 IL-6 mRNA，表明 PI3K-mTOR 通路是星形胶质细胞中 IL-6 表达的负调节因子。重要的是，Torin 2 处理未显示任何细胞毒性，因为通过 TUNEL 测定或通过蛋白质印迹法检测裂解半胱天冬酶 3 未观察到细胞死亡迹象[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    432.40

    Formula

    C24H15F3N4O
    CAS 号
    性状

    固体

    颜色

    White to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 15.62 mg/mL (36.12 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.3127 mL 11.5634 mL 23.1267 mL
    5 mM 0.4625 mL 2.3127 mL 4.6253 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.56 mg/mL (3.61 mM); 澄清溶液

      此方案可获得 ≥ 1.56 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 15.6 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 10% 1-Methyl-2-pyrrolidinone    90% PEG300

      Solubility: ≥ 2 mg/mL (4.63 mM); 澄清溶液

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.65%

    COA (290 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    HCT116 cells are treated with 100 nM Torin 2 or AZD8055 for 1 hour before they are thoroughly washed out by 3×PBS and 1×DMEM medium. Then cells are incubated in DMEM medium for indicated time before they are lysed and collected using M-PER. Protein concentrations are measured and equal amount of proteins are loaded. Experiments are repeated three times and one set of results[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][3]

    Mice[1]
    Six-week old male C57BL/6 mice are fasted overnight prior to Torin 2 treatment. The mice are treated with vehicle (for 10 h) or Torin 2 (20 mg/kg for 6h) via oral gavage and then re-fed 1 h prior to sacrifice (CO2 asphyxiation). Liver and lung are collected and frozen on dry ice. The frozen tissue is thawed on ice and lysed by sonication in tissue lysis buffer (50 mM HEPES, pH 7.4, 40 mM NaCl, 2 mM EDTA, 1.5 mM sodium orthovanadate, 50 mM sodium fluoride, 10 mM sodium pyrophosphate, 10 mM sodium β-glycerophosphate, 0.1% SDS, 1.0% sodium deoxycholate, and 1.0% Triton, supplemented with protease inhibitor cocktail tablets). The concentration of clear lysate is measured using the Bradford assay and samples are subsequently normalized by protein content and analyzed by SDS-PAGE and immunoblotting.
    Rats[3]
    Female rats (220 g) are group-housed 4 animals per cage, and kept on a 12-hour light/dark cycle with food and water ad libitum. Spinal cord injury is done with the Keck Center for Neurosciences impactor using a 10 g weight dropped from a height of 25 mm onto the dorsal surface of the exposed spinal cord. After recording BBB scores, withdrawal thresholds evoked by touch stimulus, and body weights for the first week post-injury, animals are divided into 5 treatment groups: naïve (N=4), sham (N=6), vehicle (N=6), Torin 2 (N=6), and Torin 2+Rapamycin (N=8). Torin 2 alone (4 mg/kg) or in combination with Rapamycin (1.5 mg/kg) is administered orally by gavage once a day starting at day 15 after injury and ending at day 29. In sham operated rats only the laminectomy is performed.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Torin 2 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3127 mL 11.5634 mL 23.1267 mL 57.8168 mL
    5 mM 0.4625 mL 2.3127 mL 4.6253 mL 11.5634 mL
    10 mM 0.2313 mL 1.1563 mL 2.3127 mL 5.7817 mL
    15 mM 0.1542 mL 0.7709 mL 1.5418 mL 3.8545 mL
    20 mM 0.1156 mL 0.5782 mL 1.1563 mL 2.8908 mL
    25 mM 0.0925 mL 0.4625 mL 0.9251 mL 2.3127 mL
    30 mM 0.0771 mL 0.3854 mL 0.7709 mL 1.9272 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Torin 21223001-51-1Torin2Torin-2mTORDNA-PKAutophagyApoptosisMammalian target of RapamycinDNA-dependent protein kinaseInhibitorinhibitorinhibit

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