Tomivosertib

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].

Product Specifications

CAS Number

[1849590-01-7]

Product Name Alternative

EFT508

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

MNK; PD-1/PD-L1

Type

Reference compound

Related Pathways

Immunology/Inflammation; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/eFT508.html

Purity

99.92

Solubility

DMSO : 8 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C17H20N6O2

Molecular Weight

340.38

Precautions

H315, H319, H335

References & Citations

[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.