1. MAPK/ERK Pathway
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  3. Tomivosertib

Tomivosertib (Synonyms: eFT508)

Cat. No.: HY-100022 Purity: 99.49%
Handling Instructions

Tomivosertib (eFT508) is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms.

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 1 publication(s) in Google Scholar

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Description

Tomivosertib (eFT508) is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms.

IC50 & Target[1]

MNK1

1-2 nM (IC50)

MNK2

1-2 nM (IC50)

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].

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 ibrutinib and venetoclax, in human lymphoma models[1].

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

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

Purity: 99.49%

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Tomivosertib
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HY-100022
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