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Selumetinib | Selumetinib : Covalent, ATP noncompetitive inhibitor of MAP2K1
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
MAP2K1
  • IC50:14 nM
  • IC50:10 nM
Covalent Inhibitor
10 nM - 200 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
No activity was detected with 10 uM Selumetinib against 40 kinases.

Potency
Cellular
In Vitro

MAP2K1

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1078-0432.CCR-06-1150

In Vivo Validations

Mouse
Dose: 10-100 mg/kg
Route of delivery: Oral
Organ of interest (O): xenograft
Target engagement assay: Indirect: inhibition of substrate phosphorylation in xenograft tissue

DOI Reference: 10.1158/1078-0432.CCR-06-1150

Orthogonal Probes def

TRAMETINIB

Chemical Information

Molecular Formula C17H15BrClFN4O3
SMILEs Cn1cnc2c(F)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCCO)cc21
InChI InChI=1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)
Molecular weight 456.00 Da
AlogP 3.5256000000000016
HBond acceptors 7
HBond donors 3
Atoms 42

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Expert Reviews

by SERP
(on 12 Jun 2016 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 23 Jun 2016 )
Cellular Use Rating
In Model Organisms
Selumetinib has anti-proliferative activity in cell line harboring B-RAF and RAS mutations and inhibits MEK1/2 (14 nM). It is relatively selective when tested against a panel of kinases, and commercially...
by SERP
(on 27 Jun 2016 )
Cellular Use Rating
In Model Organisms
This probe is an allosteric, non-ATP competitive and selective inhibitor of MEK1/2 kinase, a component of RAS-RAF-MEK-ERK growth pathway. It displays a remarkable selectivity for MEK1/2 with IC50 14...
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