1. MAPK/ERK Pathway Immunology/Inflammation
  2. MNK PD-1/PD-L1
  3. Tomivosertib

Tomivosertib  (Synonyms: eFT508)

Cat. No.: HY-100022 Purity: 99.92%
COA Handling Instructions

Tomivosertib (eFT508) est un inhibiteur puissant, hautement sélectif de MNK1 et de MNK2 et oralement actif, avec IC50s de 1-2 nM contre les deux isoformes. Le traitement au tomivosertib (eFT508) entraîne une réduction dose-dépendante de la phosphorylation de eIF4E à la sérine 209 (IC50=2-16 nM) dans les lignées cellulaires tumorales. Tomivosertib (eFT508) régule également considérablement l'abondance des protéines PD-L1.

Tomivosertib (eFT508) ist ein potenter, hochselektiver und oral aktiver MNK1 und MNK2-Inhibitor mit IC50s von 1-2 nM gegen beide Isoformen. Die Behandlung mit Tomivosertib führt zu einer dosisabhängigen Reduktion der eIF4E-Phosphorylierung bei Serin 209 (IC50=2-16 nM) in Tumorzelllinien. Tomivosertib reguliert auch die PD-L1-Proteinhäufigkeit dramatisch herunter.

Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance.

For research use only. We do not sell to patients.

Tomivosertib Chemical Structure

Tomivosertib Chemical Structure

CAS No. : 1849590-01-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 230 In-stock
Solution
10 mM * 1 mL in DMSO USD 230 In-stock
Solid
1 mg USD 75 In-stock
5 mg USD 210 In-stock
10 mg USD 310 In-stock
50 mg USD 950 In-stock
100 mg USD 1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Tomivosertib purchased from MedChemExpress. Usage Cited in: Oncogene. 2021 Feb 9.  [Abstract]

    Protein levels of eIF4E and MCL1 in LPS141 and MESSA cells upon treatment with eFT508 (30 μM, 24 h). The result indicates a inhibition of p-4E at 30 μM.

    View All MNK Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines[1]. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance[2].

    IC50 & Target[1]

    MNK1

    1-2 nM (IC50)

    MNK2

    1-2 nM (IC50)

    PD-L1

     

    In Vitro

    Tomivosertib (eFT508) reduces eIF4E phosphorylation dose-dependently at serine 209 (IC50=2-16 nM) in tumor cell lines. In a panel of appr 50 hematological cancers, Tomivosertib shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to Tomivosertib in TMD8, OCI-Ly3 and HBL1 DLBCL cell lines is associated with dose-dependent decreases in production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10. Further evaluation Tomivosertib mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life[1].

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

    In Vivo

    Tomivosertib (eFT508) shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, Tomivosertib combines effectively with components of R-CHOP and with novel targeted agents, including PCI-32765 and Venetoclax, in human lymphoma models[1].

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

    Clinical Trial
    Molecular Weight

    340.38

    Formula

    C17H20N6O2

    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 4.35 mg/mL (12.78 mM; Need ultrasonic; 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 2.9379 mL 14.6895 mL 29.3789 mL
    5 mM 0.5876 mL 2.9379 mL 5.8758 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.

    • 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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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: ≥ 0.44 mg/mL (1.29 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.44 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 (4.4 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.43 mg/mL (1.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (4.3 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.
    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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    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation

    Purity: 99.92%

    References

    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 2.9379 mL 14.6895 mL 29.3789 mL 73.4473 mL
    5 mM 0.5876 mL 2.9379 mL 5.8758 mL 14.6895 mL
    10 mM 0.2938 mL 1.4689 mL 2.9379 mL 7.3447 mL
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    Tomivosertib Related Classifications

    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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    Product Name:
    Tomivosertib
    Cat. No.:
    HY-100022
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