Tomivosertib (eFT-508)

Catalog No.S8275

Tomivosertib (eFT-508) Chemical Structure

Molecular Weight(MW): 340.38

Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth.

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Biological Activity

Description Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth.
Targets
MNK2 [1]
(Cell-free assay)
MNK1 [1]
(Cell-free assay)
1 nM 2.4 nM
In vitro

eFT508 has a half-maximal inhibitory concentration (IC50) of 1-2 nM against both MNK isoforms in enzyme assays and inhibits the kinase through a reversible, ATP-competitive mechanism of action. Treatment of tumor cell lines with eFT508 leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, eFT508 shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to eFT508 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[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TMD8 MXnGeY5kfGmxbjDhd5NigQ>? M{TXcFAvODFuIECuNUwhOSxiMzDhcoQhOTBizszN Mlq0NkBp MkHKdI91\W62IHTvd4Uu\GWyZX7k[Y51KGmwaHnibZRqd25ib3[g[WlHPEViU3XyNlA6KHCqb4PwbI9zgWyjdHnvci=> NED1U2kzQTV{NkC5PC=>
TMD8 M1fpNXBzd2yrZnXyZZRqd25iYYPzZZk> MXKxNkBp NIXXUJRKSzVyPUKuOVMh|ryP NGjENXM{ODh{NEG2Oy=>
MV4-11 NGLCeGxRem:uaX\ldoF1cW:wIHHzd4F6 NGfJN|IyOiCq MXLJR|UxRTF2LkS5JO69VQ>? MYqzNFgzPDF4Nx?=
K562  MkDiVJJwdGmoZYLheIlwdiCjc4PhfS=> NGj6eoEyOiCq M3\0S2lEPTB;MUOuOVQh|ryP M2rkbFMxQDJ2MU[3

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-eIF4E; 

PubMed: 30459229     


eFT508 significantly reduced the level of eIF4E phosphorylation at 0.1 and 1 μM after 1 hr, without affecting other signaling pathways in cultured mouse DRG neurons. 

30459229
Growth inhibition assay
Cell viability; 

PubMed: 30832411     


Head-to-head antiproliferative effects of VNLG-152R and eFT508 on MDA-MB-231 and MDA-MB-468 cells. The dose-response curves were generated from MTT assays after 6-day exposure to different concentrations of the compounds. Each point is a mean of replicates from three independent experiments.

30832411
In vivo

eFT508 is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of eFT508 is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations[1].

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: TMD8 cells
  • Concentrations: 0.01, 0.1, 1, 3, 10 μM
  • Incubation Time: 24 h
  • Method:

    TMD8 cells are treated with the indicated concentrations of eFT508 for 24 h. Cell lysates are subjected to m7-GTP Sepharose pull-down and bound proteins are analyzed by immunoblotting with the indicated antibodies.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL (38.19 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 340.38
Formula

C17H20N6O2

CAS No. 1849590-01-7
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID