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

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

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TAK-733 構造式

TAK-733 構造式

CAS 番号 : 1035555-63-5

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無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 166 在庫あり
Solution
10 mM * 1 mL in DMSO USD 166 在庫あり
Solid
5 mg USD 150 在庫あり
10 mg USD 277 在庫あり
50 mg USD 818 在庫あり
100 mg   お問い合わせ  
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カスタマーレビュー

Based on 5 publication(s) in Google Scholar

TAK-733 関連抗体

Top Publications Citing Use of Products

    TAK-733 purchased from MedChemExpress. 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.

    MEK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    MEK1 MEK2 MEK5 MEK

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    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)

    体外実験

    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].

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

    TAK-733 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    504.23

    分子式

    C17H15F2IN4O4
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C1C(C(NC2=CC=C(I)C=C2F)=C(F)C(N3C)=O)=C3N=CN1C[C@@H](O)CO
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 33 mg/mL (65.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1983 mL 0.9916 mL 1.9832 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 98.31%

    COA (250 KB) LCMS (95 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    TAK-733 Related Classifications

    • Molarity Calculator

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

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    • 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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    製品名:
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    製品番号:
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