Home MAPK MNK inhibitor - eIF inhibitor - PD-1/PD-L1 inhibitor Tomivosertib (eFT-508) For research use only.

Tomivosertib (eFT-508)

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. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.

Tomivosertib (eFT-508) Chemical Structure

Tomivosertib (eFT-508) Chemical Structure

CAS No. 1849590-01-7

Purity & Quality Control

Batch: S827501 DMSO]13 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.98%
99.98

Tomivosertib (eFT-508) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TMD8 Function assay 0.01, 0.1, 1, 3 and 10 μM 2 h potent dose-dependent inhibition of eIF4E Ser209 phosphorylation 29526098
TMD8 Proliferation assay 12 h IC50=2.53 μM 30824167
MV4-11 Proliferation assay 12 h IC50=14.49 μM 30824167
K562  Proliferation assay 12 h IC50=13.54 μM 30824167
Vero E6 Antiviral assay 48 h IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 0.34674 μM. 32353859
Click to View More Cell Line Experimental Data

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. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.
Targets
MNK2 [1]
(Cell-free assay)		 MNK1 [1]
(Cell-free assay)
1 nM 2.4 nM
In vitro
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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-eIF4E 30459229
Growth inhibition assay Cell viability 30832411
In Vivo
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05744739 Recruiting
Acute Myeloid Leukemia
Northwestern University|National Cancer Institute (NCI)|EFFECTOR Therapeutics Inc.
 September 29 2023 Phase 1
NCT04261218 Completed
Breast Cancer
Translational Research in Oncology|Effector Therapeutics|Stand Up To Cancer
 August 25 2020 Phase 1
NCT02937675 Terminated
Lymphoma
Effector Therapeutics
 February 8 2017 Phase 1|Phase 2
NCT02605083 Terminated
Cancer
Effector Therapeutics
 December 3 2015 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 340.38 Formula

C17H20N6O2
CAS No. 1849590-01-7 SDF Download Tomivosertib (eFT-508) SDF
Smiles CC1=C2C(=O)NC3(N2C(=O)C(=C1)NC4=NC=NC(=C4)N)CCCCC3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 13 mg/mL ( (38.19 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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