Cat. No.: HY-100022

Tomivosertib

(Synonyms: eFT508)

15 Cited Publications

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Based on 15 publication(s) in Google Scholar

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.

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Pureté: 99.75%
CAS No.: 1849590-01-7
Formule: C₁₇H₂₀N₆O₂
Masse moléculaire:340.38

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tomivosertib Chemical Structure

CAS No.: 1849590-01-7

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (15)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
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Activité biologique

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^[1]

MNK1

1-2 nM (IC₅₀)

MNK2

1-2 nM (IC₅₀)

PD-L1

Voir tous les produits spécifiques à Isoform MNK :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	GI₅₀	>50 μM Compound: eFT508	Antiproliferative activity against human A2780 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
A549	IC₅₀	>50 μM Compound: eFT508; 1	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
DOHH-2	IC₅₀	6.3 μM Compound: eFT508; 1	Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
HCT-116	GI₅₀	27.93 μM Compound: eFT508	Antiproliferative activity against human HCT116 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
HL-60	GI₅₀	>50 μM Compound: eFT508	Antiproliferative activity against human HL60 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
HT-29	IC₅₀	>50 μM Compound: eFT508; 1	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
K562	IC₅₀	13.54 μM Compound: eFT508	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30824167]
LN-18	IC₅₀	6.27 μM Compound: eFT508; 1	Antiproliferative activity against human LN-18 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human LN-18 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
MDA-MB-231	IC₅₀	45 μM Compound: eFT508; 1	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
MOLM-13	GI₅₀	33.04 μM Compound: eFT508	Antiproliferative activity against human MOLM13 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MOLM13 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
MV4-11	GI₅₀	9.26 μM Compound: eFT508	Antiproliferative activity against human MV4-11 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
MV4-11	IC₅₀	14.49 μM Compound: eFT508	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30824167]
PANC-1	IC₅₀	>50 μM Compound: eFT508; 1	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
PC-3	GI₅₀	>50 μM Compound: eFT508	Antiproliferative activity against human PC3 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
PC-3	IC₅₀	29.4 μM Compound: eFT508; 1	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
SK-OV-3	GI₅₀	>50 μM Compound: eFT508	Antiproliferative activity against human SKOV3 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SKOV3 cells assessed as inhibition in cell growth incubated for 72 hrs by MTT assay	[PMID: 31362920]
TMD8	IC₅₀	>50 μM Compound: eFT508; 1	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 38564512]
TMD8	IC₅₀	2.53 μM Compound: eFT508	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 30824167]

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].

MedChemExpress (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1849590-01-7
Appearance Solid
Masse moléculaire 340.38
Formule C₁₇H₂₀N₆O₂
Color Off-white to yellow
SMILES

O=C(C1=C(C)C=C(NC2=NC=NC(N)=C2)C(N13)=O)NC43CCCCC4
Synonyms

eFT508
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (15)

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Nat Chem Biol

MNK2 deficiency potentiates β-cell regeneration via translational regulation. [Abstract]

2022 Sep;18(9):942-953. PMID: 35697798

Tomivosertib purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2022 Sep;18(9):942-953. [Abstract]

Immunoblot analysis was performed on PANC-1 cell lysates to detect the expression of phosphorylated eIF4E (Ser 209; p-eIF4E), total eIF4E, and actin. These cells were treated with DMSO, CID661578, cercariaein, CGP57380, or eFT508 (Tomivosertib: 40 μM) for 6 hours.

Tomivosertib purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2022 Sep;18(9):942-953. [Abstract]

Six-day-old zebrafish larvae underwent β-cell ablation and were treated with DMSO, CID661578, eFT508, or a combination of CID661578 and eFT508 (Tomivosertib: 10 μM) for 48 hours. The number of β-cells was then quantitatively analyzed.
Brain

Tomivosertib reduces ectopic activity in dorsal root ganglion neurons from patients with radiculopathy. [Abstract]

2024 Jul 24:awae178. PMID: 39046204

Tomivosertib purchased from MedChemExpress. Usage Cited in: Brain. 2024 Jul 24:awae178. [Abstract]

MNK inhibition with eFT508 (Tomivosertib: 25 nM) rapidly decreases phosphorylated eIF4E in human dorsal root ganglion neurons. Representative enlarged images of p-eIF4E immunostaining (red) and neuronal marker, peripherin (blue).

Tomivosertib purchased from MedChemExpress. Usage Cited in: Brain. 2024 Jul 24:awae178. [Abstract]

Treatment with eFT508 (Tomivosertib: 25 nM) reverses spontaneous activity in human dorsal root ganglion neurons associated with painful dermatomes.
Clin Cancer Res

Pharmacologic inhibition of eIF4A blocks NRF2 synthesis to prevent osteosarcoma metastasis. [Abstract]

2024 Oct 1;30(19):4464-4481. PMID: 39078310
Mol Psychiatry

Correction of eIF4E overactivation rescues translatome imbalance and core ASD-like behaviors in valproic acid-induced offspring mice. [Abstract]

2026 Mar 7. PMID: 41795048
Oncogene

MNK1 and MNK2 enforce expression of E2F1, FOXM1, and WEE1 to drive soft tissue sarcoma. [Abstract]

2021 Mar;40(10):1851-1867. PMID: 33564073

Tomivosertib purchased from MedChemExpress. Usage Cited in: Oncogene. 2021 Mar;40(10):1851-1867. [Abstract]

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.
PLoS Biol

RSK1 promotes mammalian axon regeneration by inducing the synthesis of regeneration-related proteins. [Abstract]

2022 Jun 1;20(6):e3001653. PMID: 35648763
J Med Chem

Development of a Direct-to-Biology Platform to Discover Potent MNK Inhibitors. [Abstract]

2026 May 28;69(10):12543-12564. PMID: 42126237
Front Endocrinol

ZIP9 mediates the effects of DHT on learning, memory and hippocampal synaptic plasticity of male Tfm and APP/PS1 mice. [Abstract]

2023 May 25:14:1139874. PMID: 37305050
J Virol

Phospho-eIF4E stimulation regulates coronavirus entry by selective expression of cell membrane-residential factors. [Abstract]

2024 Feb 20;98(2):e0194823. PMID: 38299843
Neurobiol Pain

Interleukin-6 induces nascent protein synthesis in human dorsal root ganglion nociceptors primarily via MNK-eIF4E signaling. [Abstract]

2024 Jul 26:16:100159. PMID: 39156884
Vet Microbiol

Mechanistic link between eIF4E phosphorylation and viral pathogenesis: Therapeutic insights from a porcine model. [Abstract]

2025 Dec 15:312:110818. PMID: 41418357
bioRxiv

Live cell imaging reveals paclitaxel-induced lysosome motility and function disruption in DRG neurons. [Abstract]

2026 May 21:2026.05.19.726221. PMID: 42239088
bioRxiv

Expansion of OSMR expression and signaling in the human dorsal root ganglion links OSM to neuropathic pain. [Abstract]

2025 Apr 1:2025.03.26.645611. PMID: 40236060
bioRxiv

2024 Apr 6.
bioRxiv

MNK inhibitor eFT508 (Tomivosertib) suppresses ectopic activity in human dorsal root ganglion neurons from dermatomes with radicular neuropathic pain. [Abstract]

2023 Jun 14:2023.06.13.544811. PMID: 37398249

Solvant et solubilité

In Vitro:

DMSO : 8 mg/mL (23.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[1]. Kevin R. Webster, et al. eFT508, a Potent and Selective Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 Inhibitor, Is Efficacious in Preclinical Models of Diffuse Large B-Cell Lymphoma (DLBCL). Blood 2015 126:1554.

[2]. Xu Y, et al. Translation control of the immune checkpoint in cancer and its therapeutic targeting. Nat Med. 2019 Feb;25(2):301-311. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9379 mL	14.6895 mL	29.3789 mL	73.4473 mL
	5 mM	0.5876 mL	2.9379 mL	5.8758 mL	14.6895 mL
	10 mM	0.2938 mL	1.4689 mL	2.9379 mL	7.3447 mL
	15 mM	0.1959 mL	0.9793 mL	1.9586 mL	4.8965 mL
	20 mM	0.1469 mL	0.7345 mL	1.4689 mL	3.6724 mL

Keywords

Tomivosertib

15 Cited Publications

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Tomivosertib

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

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Small Molecule Immuno-Oncology Compound Library

Drug Repurposing Compound Library

Oxygen Sensing Compound Library

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Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Tomivosertib

Voir tous les produits spécifiques à Isoform MNK

Activité biologique

Chemical Information

Publications (15)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tomivosertib Related Classifications

Cat. No.: HY-100022