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

Tomivosertib (Synonyms: eFT508)

Cat. No.: HY-100022 Purity: 99.92%
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
10 mM * 1 mL in DMSO USD 189 In-stock
Estimated Time of Arrival: December 31
1 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 252 In-stock
Estimated Time of Arrival: December 31
10 mg USD 372 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1620 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE Tomivosertib

    Tomivosertib purchased from MCE. Usage Cited in: Oncogene. 2021 Feb 9.

    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.

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    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

    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].

    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].

    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.

    1849590-01-7

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 4.35 mg/mL (12.78 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.2938 mL 1.4689 mL 2.9379 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    • 3.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: 0.4 mg/mL (1.18 mM); Suspended solution; Need ultrasonic

    • 4.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: 0.4 mg/mL (1.18 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.92%

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    Keywords:

    TomivosertibeFT508eFT 508eFT-508MNKPD-1/PD-L1Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinasePD-1/Programmed death-ligand 1Inhibitorinhibitorinhibit

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