2. MAPK/ERK Pathway
  3. MEK
  4. TAK-733

TAK-733 是一种有效的选择性 MEK 抑制剂，IC50 为 3.2 nM。

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TAK-733 Chemical Structure

TAK-733 Chemical Structure

CAS No. : 1035555-63-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1389
In-stock
2 mg ￥834
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5 mg ￥1252
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10 mg ￥2358
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50 mg 现货 询价
100 mg   询价  
200 mg   询价  

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Customer Review

TAK-733 相关抗体

Top Publications Citing Use of Products

    TAK-733 purchased from MCE. Usage Cited in: Exp Mol Med. 2018 Apr 20;50(4):37.  [Abstract]

    TAK-733 attenuates the Ang II-induced increases in cyclin D1 and PCNA protein expression.

    查看 MEK 亚型特异性产品:

    查看所有亚型
    MEK1 MEK2 MEK5 MEK

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.

    IC50 & Target[1]

    MEK

    3.2 nM (IC50)

    体外研究
    (In Vitro)

    TAK-733 exhibits potent enzymatic and cell activity with an IC50 of 3.2 nM against constitutively active MEK enzyme and an EC50 of 1.9 nM against ERK phosphorylation in cells. TAK-733 does not inhibit any other kinases, receptors or ion channels that are tested with inhibitor concentrations up to 10 μM. TAK-733 is found to bind plasma protein moderately (ca. 97% for human and 96% for mouse), and exhibits high permeability and high microsomal stability across species. It does not inhibit P450s up to 30 μM[1]. TAK-733 demonstrates broad activity in most melanoma cell lines with relative resistance observed at IC50 >0.1 μM in vitro. Thirty-four melanoma cell lines are exposed in vitro to increasing concentrations of TAK-733 for 72 hours. Of the 34 cell lines, 27 are BRAFV600E mutant and 7 are wild-type. SRB proliferation assays are performed and the resulting IC50 concentrations allowed stratification of cell lines into three categories: relatively resistant, intermediate, and highly sensitive. Relatively resistant and highly sensitive lines are assigned based on an IC50 that differ by at least 10 fold[2].

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

    TAK-733 相关抗体:
    体内研究
    (In Vivo)

    The pharmacokinetics of TAK-733 is evaluated in nude mouse, rat, dog and monkey. Low clearance and high oral bioavailability are observed in all species. TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer[1]. Daily oral administration of 1, 3, 10, and 30 mg/kg of TAK-733 for 14 days (Days 10 to 23) results in tumor growth delay in the A375 cell-implanted mice (5/group). TAK-733 (35, 70, 100, and 160 mg/kg) also significantly inhibits tumor growth on an intermittent dosing schedule of 3 days per week for 2 weeks (Days 10, 13, 15, 17, 20, and 22). Three partial regressions (PR), a 60% response rate, are observed in mice administered with 30 mg/kg of TAK-733 daily and in mice administered with 160 mg/kg of TAK-733 intermittently. Responses, CR (complete regression) and partial regressions (PR) are also observed in mice administered with 70, 100, and 160 mg/kg of TAK-733 intermittently. The tumor regression rate is more pronounced with the intermittent administration regimen; the greatest reduction in tumor volume is observed at 160 mg/kg (57.29%), versus a maximum reduction of 46.97% at 30 mg/kg once daily. By the last day of administration, tumor growth is significantly (p<0.05 for %T/C, Student's t-test) inhibited in mice administered 3, 10, and 30 mg/kg once daily or 35, 70, 100, and 160 mg/kg intermittently[2].

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

    504.23

    Formula

    C17H15F2IN4O4
    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 33 mg/mL (65.45 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9832 mL 9.9161 mL 19.8322 mL
    5 mM 0.3966 mL 1.9832 mL 3.9664 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.96 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，此方案实验周期在半个月以上的动物实验酌情使用。

      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玉米油中，混合均匀。

    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: 98.31%

    COA (193 KB) LCMS (95 KB)

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

    The cutaneous melanoma cell lines in logarithmic growth phase are transferred to 96 well flat bottom plates with lids. One hundred μL cell suspensions containing 2000-3000 viable cells are plated into each well and incubated overnight prior to exposure with increasing concentrations of TAK-733 (10, 20, 30, 40, 50, 60, 70, 80, 90, and 100 nM) for 72 hours. Post drug administration, media is removed and cells are fixed with cold 10% trichloroacetic acid for 30 min. at 4°C. Cells are then washed with water and stained with 0.4% SRB for 30 min at room temperature, washed again with 1% acetic acid, followed by stain solubilization with 10 mM tris at room temperature. The absorbance at 565 nm is measured on a plate reader. Cell proliferation curves are derived from the raw absorbance (OD) data. Statistical analyses and graphical representation of data are using GraphPad Prism version 5.00[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Five to six-week-old female athymic nude mice are used. A375 human melanoma xenograft tumors are generated by harvesting cells from mid-log phase cultures using Trypsin-EDTA. Approximately 5×106 cells suspended in Hanks’ balanced salt solution (HBSS) are injected sc into the right flank of 6-8-week-old mice. Oral administration of TAK-733 (1 mg/kg or 10 mg/kg) is initiated when tumors in all mice in each experiment range in size from 100 to 200 mm3 for antitumor efficacy studies and from 300 to 500 mm3 for pharmacodynamic (PD) studies[2].

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

    TAK-733 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9832 mL 9.9161 mL 19.8322 mL 49.5805 mL
    5 mM 0.3966 mL 1.9832 mL 3.9664 mL 9.9161 mL
    10 mM 0.1983 mL 0.9916 mL 1.9832 mL 4.9581 mL
    15 mM 0.1322 mL 0.6611 mL 1.3221 mL 3.3054 mL
    20 mM 0.0992 mL 0.4958 mL 0.9916 mL 2.4790 mL
    25 mM 0.0793 mL 0.3966 mL 0.7933 mL 1.9832 mL
    30 mM 0.0661 mL 0.3305 mL 0.6611 mL 1.6527 mL
    40 mM 0.0496 mL 0.2479 mL 0.4958 mL 1.2395 mL
    50 mM 0.0397 mL 0.1983 mL 0.3966 mL 0.9916 mL
    60 mM 0.0331 mL 0.1653 mL 0.3305 mL 0.8263 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:

    TAK-7331035555-63-5TAK733TAK 733MEKMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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    目录号：
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