tomivosertib   Click here for help

GtoPdb Ligand ID: 10167

Synonyms: compound 23 [PMID: 29526098] | eFT-508 | eFT508
PDB Ligand Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Tomivosertib (eFT508) is an orally active and selective mitogen-activated protein kinase interacting kinases 1 and 2 (MNK1/2) inhibitor that is being developed by eFFECTOR Therapeutics for anti-neoplastic potential [2].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 6
Hydrogen bond donors 3
Rotatable bonds 2
Topological polar surface area 114.93
Molecular weight 340.16
XLogP 2.41
No. Lipinski's rules broken 0
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Canonical SMILES Nc1ncnc(c1)Nc1cc(C)c2n(c1=O)C1(CCCCC1)NC2=O
Isomeric SMILES Nc1ncnc(c1)Nc1cc(C)c2n(c1=O)C1(CCCCC1)NC2=O
InChI InChI=1S/C17H20N6O2/c1-10-7-11(21-13-8-12(18)19-9-20-13)16(25)23-14(10)15(24)22-17(23)5-3-2-4-6-17/h7-9H,2-6H2,1H3,(H,22,24)(H3,18,19,20,21)
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Summary of Clinical Use Click here for help
Tomivosertib has advanced to Phase 2 clinical evaluation, with active trials investigating its effect in solid tumours. A Phase 1/2 trial in lymphoma was terminated. Click here to link to's full list of tomivosertib trials.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
MNK1 and 2 phosphorylate the mRNA binding protein eIF4E to mediate regulation of RNA translation. Pharmacological inhibition of MNK1/2 reduces translation of a subset of mRNAs that control tumour and stromal cell activity, and produces an anti-tumourigenic effect.