Tomivosertib |
Inhibitor of MKNK1, MKNK2
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| MKNK1 |
|
|
| MKNK2 |
|
|
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 (IV)-10 (PO) mg/Kg
Route of delivery:
Intravenous, Oral
Plasma half life:
5.3 h (PO)
Systemic clearance:
33 ml/min/Kg (IV)
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 |
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