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SGX-523 | SGX-523 : ATP competitive inhibitor of MET
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

Targets Biochemical/Biophysical Potency Cellular Potency
MET
  • Ki:2.7 nM
  • IC50:12 nM
ATP competitive
1 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - RON ~10 uM

Potency Assay Off-Target:
At 1,000 nM, SGX-523 did not inhibit any of 213 kinases >36%, making it at least 1,000-fold selectiv ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
SGX-523 did not effect phosphorylation of substrates of RON or 8 other kinases.

Potency
Cellular
In Vitro

MET

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 158/1535-7163.MCT-09-0477

Orthogonal Probes def

AMG 337
Capmatinib
MK-8033

Chemical Information

Molecular Formula C18H13N7S
SMILEs Cn1cc(-c2ccc3nnc(Sc4ccc5ncccc5c4)n3n2)cn1
InChI InChI=1S/C18H13N7S/c1-24-11-13(10-20-24)16-6-7-17-21-22-18(25(17)23-16)26-14-4-5-15-12(9-14)3-2-8-19-15/h2-11H,1H3
Molecular weight 359.10 Da
AlogP 3.2242000000000006
HBond acceptors 7
HBond donors --
Atoms 39

References

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Cross References

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Expert Reviews

by SERP
(on 2 Jun 2016 )
Cellular Use Rating
In Model Organisms
In vitro potency data against MET are for the kinase domain only and not the full-length enzyme.
by SERP
(on 20 Jun 2016 )
Cellular Use Rating
In Model Organisms
SGX523 potently inhibited MET with an IC50 of 4 nM and is >250-fold selective versus 213 other protein kinases, representing approximately half of all catalytically competent human protein kinases and...
From a chemists point of view, this compound is a good probe.
by SERP
(on 21 Dec 2016 )
Cellular Use Rating
In Model Organisms
This is an excellent probe molecule. It was highlighted in the famous Nature Biotechnology kinase inhibitor article (Nature Biotechnology 2011, 29, 1046–1051) as one of the most selective kinase inhibitors...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria