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 NXvBW3d1TnWwY4Tpc44h[XO|YYm= NFHjNY8xNjBzLDCwMlEtKDFuIEOgZY5lKDFyIN88US=> NIjVXXUzKGh? NF\E[m5xd3SnboSg[I9{\S2mZYDlcoRmdnRiaX7obYJqfGmxbjDv[kBmUUZ2RTDT[ZIzODlicHjvd5Bpd3K7bHH0bY9v MoX6Nlk2OjZyOUi=
TMD8 M1LubXBzd2yrZnXyZZRqd25iYYPzZZk> NWLMVlU2OTJiaB?= MUfJR|UxRTJwNUOg{txO Mmi5N|A5OjRzNke=
MV4-11 MlnaVJJwdGmoZYLheIlwdiCjc4PhfS=> NUDjRVZuOTJiaB?= NID3WFFKSzVyPUG0MlQ6KM7:TR?= NYeyeoE2OzB6MkSxOlc>
K562  NFG2UoJRem:uaX\ldoF1cW:wIHHzd4F6 MV:xNkBp MlnVTWM2OD1zMz61OEDPxE1? MU[zNFgzPDF4Nx?=

... Click to View More Cell Line Experimental Data

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]

+ Expand
  • 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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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03690141 Recruiting Castrate-resistant Prostate Cancer (CRPC) Effector Therapeutics October 12 2018 Phase 2
NCT03690141 Recruiting Castrate-resistant Prostate Cancer (CRPC) Effector Therapeutics October 12 2018 Phase 2
NCT03616834 Recruiting Solid Tumors Effector Therapeutics July 25 2018 Phase 2
NCT03616834 Recruiting Solid Tumors Effector Therapeutics July 25 2018 Phase 2
NCT03318562 Terminated Triple Negative Breast Cancer|Hepatocellular Carcinoma Effector Therapeutics November 17 2017 Phase 2
NCT03318562 Terminated Triple Negative Breast Cancer|Hepatocellular Carcinoma Effector Therapeutics November 17 2017 Phase 2

Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID