General
Preferred name
tomivosertib
Synonyms
eFT508 ()
N45 ()
cpd 23 ()
EFT-508 ()
Tomivosertib (eFT-508) ()
Eft 508 ()
Tomivosertib hydrochloride ()
eFT508 ()
Eft508 ()
EFT-508 HYDROCHLORIDE ()
eFT508HCl ()
P&D ID
PD057001
CAS
1849590-01-7
Tags
available
probe
drug candidate
Drug indication
Triple negative breast cancer
Hepatocellular carcinoma
Neoplasm
Solid tumour/cancer
Colorectal cancer
colorectal carcinoma
Lymphoma
Drug Status
investigational
Max Phase
2.0
1.0
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
3
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
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 .
(GtoPdb)
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].
PRICE
153
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
Tomivosertib, also known as eFT508 is a MNK1/2 inhibitor. Tomivosertib binds to and inhibits the activity of MNK1 and 2. This prevents MNK1/2-mediated signaling, and inhibits the phosphorylation of certain regulatory proteins, including eukaryotic translation initiation factor 4E (eIF4E), that regulate the translation of messenger RNAs (mRNAs) involved in tumor cell proliferation, angiogenesis, survival and immune signaling
(PKIDB)
DESCRIPTION
Tomivosertib (eFT508) is a potent and highly selective MNK1 and MNK2 inhibitor with an IC50 value of 1-2 nM.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
9
Organisms
2
Compound Sets
17
AdooQ Bioactive Compound Library
Cayman Chemical Bioactives
ChEMBL Drugs
Chemical Probes.org
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
MedChem Express Bioactive Compound Library
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
26
Molecular Weight
340.16
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
3
Rotatable Bonds
2
Ring Count
4
Aromatic Ring Count
2
cLogP
1.63
TPSA
114.93
Fraction CSP3
0.41
Chiral centers
0.0
Largest ring
6.0
QED
0.77
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
MNK
MNK1
MNK2
PD-1/PD-L1
eIF,MNK,PD-1/PD-L1
MKNK1, MKNK2
MOA
MAPK-interacting kinase inhibitor
Pathway
Apoptosis
Cell Cycle/Checkpoint
Immunology/Inflammation
MAPK
MAPK/ERK Pathway
Target subclass
CAMK
CAMK, CAMK
Target class
Protein kinase
Kinase, Kinase
Recommended Cell Concentration
100 nM
Source data
