1. Stem Cell/Wnt
  2. β-catenin
  3. Tegatrabetan

Tegatrabetan  (Synonyms: Tegavivint; BC2059; テガビビント)

製品番号: HY-109103 純度: 99.84%
COA 取扱説明書 Technical Support

Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1227637-23-1

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 128 在庫あり
Solution
10 mM * 1 mL in DMSO USD 128 在庫あり
Solid
5 mg $99 在庫あり
10 mg $165 在庫あり
50 mg $473 在庫あり
100 mg $803 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26.  [Abstract]

    Images of spheroids grown in ultralow attachment plates treated with Tegavivint (Tega) (5 μM), and quantification of spheroid viability was performed with CellTiter-Glo.

    Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26.  [Abstract]

    Tegatrabetan (Tega) (10 mg/kg; i.p.; twice a week) enlonged time to tumor tripling of Foxn1nsup>u mouse xenograft tumor model.

    Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26.  [Abstract]

    Tegatrabetan (Tega) (2.5 μM) were lethal to RNF43-mutant-HPAF-IIN.

    Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26.  [Abstract]

    Tegatrabetan (Tega) (2.5 μM) were lethal to Capan-2 cells.

    Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26.  [Abstract]

    Tegavivint (Tega) (10-8-10-5 M; 48 h) caused HT-1080N cell death.
    • 生物活性

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    • 参考文献

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    製品説明

    Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1)[1].

    IC50 & Target

    β-Catenin[1]

    体外実験

    Tegatrabetan (BC2059; 20-100 nM; 48 hours) inhibits cell proliferation in suspension culture over 120 hours and induces apoptosis of cultured human acute myeloid leukemia (AML) HL-60, OCI-AML3 and MV4-11 cells dose-dependently[1].
    Tegatrabetan (20 and 50 nM; 24 hours) induces a modest but significant accumulation of cells in the G0/G1 phase, with a concomitant decline in the G2/M phase of the cell cycle[1].
    Tegatrabetan (100 nM, 24 hours) depletes the levels of β-catenin and its target genes, including c-MYC and survivin without affecting the levels of the TBL1 in OCI-AML3, HL-60 and MV4-11 cells[1].

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

    Cell Proliferation Assay[1]

    Cell Line: HL-60, OCI-AML3 and MV4-11 cells
    Concentration: 20, 50, and 100 nM
    Incubation Time: 48 hours
    Result: Dose-dependently inhibited cell proliferation.

    Cell Cycle Analysis[1]

    Cell Line: OCI-AML3 cells
    Concentration: 20 and 50 nM
    Incubation Time: 24 hours
    Result: Dose-dependently induced cell cycle growth arrest.

    Western Blot Analysis[1]

    Cell Line: OCI-AML3, HL-60 and MV4-11 cells
    Concentration: 100 nM
    Incubation Time: 24 hours
    Result: Treatment depleted β-Catenin expression levels.
    体内実験

    Tegatrabetan (BC2059; 1.0 or 5.0 mg/kg/day; intravenously) significantly improves the median survival of the mice from approximately 17.5 to 39 days. Treatment with Tegatrabetan (10 mg/kg/day; intravenously) alone further improves the median survival to 51.5 days[1].

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

    Animal Model: NOD/SCID mice bearing OCI-AML3 xenografts[1]
    Dosage: 1 mg/kg; 5 mg/kg; 10 mg/kg
    Administration: Intravenously; 1 mg/kg daily 4 days per week or 5 mg/kg or 10 mg/kg of BC2059 twice per week (Tuesday and Thursday) for 3 weeks.
    Result: Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts.
    臨床実験
    分子量

    588.74

    分子式

    C28H36N4O6S2

    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=S(C1=CC2=C(C=C1)/C(C3=CC=C(S(=O)(N4C[C@H](C)C[C@H](C)C4)=O)C=C3/C2=N\O)=N\O)(N5C[C@H](C)C[C@H](C)C5)=O

    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 : 50 mg/mL (84.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6985 mL 8.4927 mL 16.9854 mL
    5 mM 0.3397 mL 1.6985 mL 3.3971 mL
    10 mM 0.1699 mL 0.8493 mL 1.6985 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます:C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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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: 99.84%

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6985 mL 8.4927 mL 16.9854 mL 42.4636 mL
    5 mM 0.3397 mL 1.6985 mL 3.3971 mL 8.4927 mL
    10 mM 0.1699 mL 0.8493 mL 1.6985 mL 4.2464 mL
    15 mM 0.1132 mL 0.5662 mL 1.1324 mL 2.8309 mL
    20 mM 0.0849 mL 0.4246 mL 0.8493 mL 2.1232 mL
    25 mM 0.0679 mL 0.3397 mL 0.6794 mL 1.6985 mL
    30 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4155 mL
    40 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0616 mL
    50 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8493 mL
    60 mM 0.0283 mL 0.1415 mL 0.2831 mL 0.7077 mL
    80 mM 0.0212 mL 0.1062 mL 0.2123 mL 0.5308 mL
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    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
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    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.

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    製品名:
    Tegatrabetan
    製品番号:
    HY-109103
    数量:
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