2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Anti-infection
  3. DNA/RNA Synthesis Akt HIV
  4. Triciribine

Triciribine  (Synonyms: 曲西立滨; API-2; NSC 154020; TCN)

目录号: HY-15457 纯度: 98.59%
COA 产品使用指南

摩尔计算器

Triciribine 是一种 DNA 合成 (DNA synthesis) 抑制剂，也抑制 Akt 和 HIV-1/2，IC50 分别为 130 nM 和 0.02-0.46 μM。

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Triciribine Chemical Structure

Triciribine Chemical Structure

CAS No. : 35943-35-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥921
In-stock
1 mg ￥380
In-stock
5 mg ￥837
In-stock
10 mg ￥1150
In-stock
50 mg ￥3800
In-stock
100 mg ￥5850
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Triciribine:

Triciribine 相关抗体

Top Publications Citing Use of Products

    Triciribine purchased from MCE. Usage Cited in: Stem Cell Res Ther. 2018 Mar 1;9(1):52.  [Abstract]

    Signaling protein expression detected by western blotting and quantified by densitometry with or without Triciribine.

    Triciribine purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290.  [Abstract]

    API-2 apparently inhibits insulin induced phosphorylation of Akt S473 in a dose dependent manner.

    Triciribine purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290.  [Abstract]

    Inhibition of pAkt by API-2 effectively prevents K145 induced increasing phosphorylation of FoxO1 in response to insulin. API-2 also significantly reverses K145 suppressed PEPCK and G6Pase mRNA and protein expression.

    查看 Akt 亚型特异性产品:

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    Akt Akt1 Akt2 Akt3

    查看 HIV 亚型特异性产品:

    查看所有亚型
    HIV HIV-1 HIV-2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively.

    IC50 & Target[1][2][3]

    DNA synthesis

     

    HIV-1

    0.02-0.46 μM (IC50)

    HIV-2

    0.02-0.46 μM (IC50)

    Akt

    130 nM (IC50, cell assay)

    体外研究
    (In Vitro)

    The nucleoside analog Triciribine (TCN) is a purine analog which is initially shown to inhibit DNA synthesis. Triciribine selectively inhibits the phosphorylation and activation of all three Akt isoforms. At a concentration of 10 μM Triciribine Akt phosphorylation is inhibited at both Thr308 and Ser473. Triciribine effectively inhibits the phosphorylation and consequently the catalytic activity of Akt in PC-3 cells[1]. The Akt inhibitor Triciribine (TCN) does not effectively inhibit the human cell line U87MG but inhibits other astrocytoma cell lines in a grade-dependent manner. The WHO II K1861-10 line is incompletely inhibited (69% maximum inhibition) with a GI50 value of 1.7 μM for Triciribine. Triciribine exhibits maximum growth inhibition around 1-10 μM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100 μM (IC50=130 nM) in KR158 cells[2]. Triciribine (TCN) is a novel tricyclic compound with known antitumor activity. Using a syncytial plaque assay, Triciribine is active against HIV-1 at 0.01-0.02 μM. Using a microtiter XTT assay, Triciribine is active against a panel of HIV-1 and HIV-2 strains at IC50 values ranging from 0.02 to 0.46 μM[3].

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

    Triciribine 相关抗体:
    体内研究
    (In Vivo)

    Triciribine (TCBN) treatment, administered for 7 days after 14 days of hypoxia until 21 days of hypoxia is reached, reversed the vascular thickening as shown by immunohistochemistry and Western analyses. On the other hand, Rapamycin treatment did not prevent hypoxia-induced pulmonary alveolar haemorrhage and congestion. Triciribine partially inhibits progressive pruning of the vasculature[4].

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

    320.30

    Formula

    C13H16N6O4
    CAS 号
    性状

    固体

    颜色

    Light yellow to khaki

    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 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (312.21 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 3.1221 mL 15.6104 mL 31.2207 mL
    5 mM 0.6244 mL 3.1221 mL 6.2441 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1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: ≥ 2.5 mg/mL (7.81 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.81 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    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: 99.81%

    COA (198 KB) LCMS (112 KB)

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

    The human SF295 and U87MG GBM lines and the mouse K1861-10, KR158, and KR130G astrocytoma lines are plated at a density of 2500 cells/100 µL complete media in 96-well plates. Mouse primary astrocytes are plated at 5000 cells/100 µL. Cells are treated in triplicate with serial dilutions of inhibitors (The inhibitors tested are PI-103, Triciribine and Rapamycin) ranging from µM to pM. Cell proliferation is measured after 3 days using the Alamar Blue assay on a Novostar plate reader. Values for 50% inhibitory concentration (IC50) and 50% growth inhibitory concentration (GI50) are calculated using standard procedures in GraphPad Prism v4 and Microsoft Excel[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Mice[4]
    Akt1+/+ and Akt1−/− mice are subjected to normoxia or hypoxia (10% O2) for 7 and 14 days (n=2-6 mice per group). Noteworthy, high mortality is observed in Akt1−/− mice exposed to hypoxia longer than 14-16 days. For pharmacological inhibition studies, Akt1+/+ mice, subjected to normoxia or chronic hypoxia for 14 days, received daily i.p. injection of saline, Triciribine (0.5 mg/kg per day) or Rapamycin (1.5 mg/kg per day) for 7 days, and the total continuous exposure to hypoxia or normoxia is 21 days (n=6-8 mice per group). Pharmacological inhibitors are administered daily while the mice are maintained in the hypoxia chamber to minimize exposure to air and spontaneous reversal of pulmonary remodelling.

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

    Triciribine 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1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 3.1221 mL 15.6104 mL 31.2207 mL 78.0518 mL
    5 mM 0.6244 mL 3.1221 mL 6.2441 mL 15.6104 mL
    10 mM 0.3122 mL 1.5610 mL 3.1221 mL 7.8052 mL
    15 mM 0.2081 mL 1.0407 mL 2.0814 mL 5.2035 mL
    20 mM 0.1561 mL 0.7805 mL 1.5610 mL 3.9026 mL
    25 mM 0.1249 mL 0.6244 mL 1.2488 mL 3.1221 mL
    30 mM 0.1041 mL 0.5203 mL 1.0407 mL 2.6017 mL
    40 mM 0.0781 mL 0.3903 mL 0.7805 mL 1.9513 mL
    50 mM 0.0624 mL 0.3122 mL 0.6244 mL 1.5610 mL
    60 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3009 mL
    80 mM 0.0390 mL 0.1951 mL 0.3903 mL 0.9756 mL
    100 mM 0.0312 mL 0.1561 mL 0.3122 mL 0.7805 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:

    Triciribine35943-35-2API-2 NSC 154020 TCNAPI2API 2NSC154020NSC 154020NSC-154020DNA/RNA SynthesisAktHIVPKBProtein kinase BHuman immunodeficiency virusInhibitorinhibitorinhibit

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    目录号：
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