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Tomivosertib | Inhibitor of MKNK1, MKNK2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
MKNK1
  • IC 50:2.4 nM
  • IC 50:6 nM
MKNK2
  • IC 50:1 nM
  • IC 50:6 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - STK17A 130 nM, CLK4 790 nM

Selectivity Assessment Description:
Profiled for kinase selectivity at 1 uM over 400 kinases showing only 2 off-targets
In Cell Selectivity Assessment
Selectivity Assessment Description:
Tomivosertib did not show antiproliferative activity in a panel of solid and hematological t ...

Potency
Cellular
In Vitro

MKNK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.7b01795

MKNK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.7b01795

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 5.3 h (PO)
Systemic clearance: 33 ml/min/Kg (IV)
Volume of Distribution at Steady-State: 2.9

DOI Reference: 10.1021/acs.jmedchem.7b01795

Dose: 10 mg/ Kg
Route of delivery: Oral
Cmax: 1.0 µg/mL
Tmax: 1.0 h
Area Under the Curve:: 4.0 h*µg/mL

DOI Reference: 10.1021/acs.jmedchem.7b01795

Rat
Dose: 10 mg/kg
Route of delivery: Oral
Fb : 85%

DOI Reference: 10.1021/acs.jmedchem.7b01795

Monkey (Cynomolgus)
Dose: 3mg/kg
Route of delivery: Oral
Fb : 24%

DOI Reference: 10.1021/acs.jmedchem.7b01795

Dog
Dose: 5 mg/kg
Route of delivery: Oral
Fb : >100 %

DOI Reference: 10.1021/acs.jmedchem.7b01795

Chemical Information

Molecular Formula C17H20N6O2
SMILEs Cc1cc(Nc2cc(N)ncn2)c(=O)n2c1C(=O)NC21CCCCC1
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)
Molecular weight 340.16 Da
AlogP 1.6328199999999995
HBond acceptors 8
HBond donors 4
Atoms 45

Vendors

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Expert Reviews

by SERP
(on 26 Aug 2024)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 6 Sept 2024)
Cellular Use Rating
In Model Organisms
eFT508 / Tomivosertib is a well characterized balanced single digit nanomolar inhibitor of MKNK1 (= MNK1) and MKNK2 (= MNK2). High selectivity was proven in a kinome selectivity screen at 1 µM compound...
by SERP
(on 27 May 2026)
Cellular Use Rating
In Model Organisms
eFT508 / Tomivosertib is a excellent inhibitor of MKNK1 and MKNK2 showing significant selectivity and potency. High selectivity was shown in a kinome-wide selectivity screen at 1 µM compound concentration,...
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