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MK-8033 | MK-8033 : ATP competitive inhibitor of MET and MST1R
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MET
  • IC 50:1 nM
  • Kd:3.2 nM
  • IC50:29 nM
MST1R
  • IC50:7 nM
  • IC 50:580 nM
ATP competitive
1-10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Kinase selectivity @ 1 μmol/L was tested using 221 kinases by Millipore and only MET and MST1R, we ...

Potency
Cellular
In Vitro

MET

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm301619u

MST1R

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm301619u

In Vivo Validations

Rat, Dog
Dose: 10, 30, 100 mg/Kg
Route of delivery: Oral
Plasma half life: 0.8 (R), 3.1 (D) h
Systemic clearance: 20 (R), 3.1 (D) mL/min/Kg

DOI Reference: 10.1021/jm301619u

Orthogonal Probes def

CAPMATINIB
SGX-523
AMG-337

Chemical Information

Molecular Formula C25H21N5O3S
SMILEs Cn1cc(-c2cnc3ccc4ccc(CS(=O)(=O)NCc5ccccn5)cc4c(=O)c3c2)cn1
InChI InChI=1S/C25H21N5O3S/c1-30-15-20(13-28-30)19-11-23-24(27-12-19)8-7-18-6-5-17(10-22(18)25(23)31)16-34(32,33)29-14-21-4-2-3-9-26-21/h2-13,15,29H,14,16H2,1H3
Molecular weight 471.14 Da
AlogP 0.0
HBond acceptors 8
HBond donors 1
Atoms 55

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 19 Jun 2021 )
Cellular Use Rating
In Model Organisms
The compound is a potent dual-active cMET-MST1R (Ron) kinase inhibitor. >100 fold selectivity vs a broad kinome panel is presented, but no other broad selectivity is shown. The molecule is 7 fold...
by SERP
(on 15 Aug 2021 )
Cellular Use Rating
In Model Organisms
MK-8033 has preferential binding to the activated kinase conformation of the MET protein.
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