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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
Vendors
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Probe Summary

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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 public 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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