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AMG-337 | AMG-337 : 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
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MET
  • IC50:1 nM
  • IC50:5 nM
ATP competitive
100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
competitive binding assays illustrated the selectivity of AMG 337, binding only MET when profiled ...

Potency
Cellular
In Vitro

MET

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5b01716

In Vivo Validations

Mouse, Rat
Dose: 0.1-10 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 3 h
Systemic clearance: 0.27 (IV), 1.6 (PO) L/h/Kg

DOI Reference: 10.1021/acs.jmedchem.5b01716

Orthogonal Probes def

CAPMATINIB
SGX-523
MK-8033

Chemical Information

Molecular Formula C24H24FN7O2
SMILEs C=C1c2cc(OCCOC)cnc2C=CN1C(C)c1nnc2c(F)cc(-c3cnn(C)c3)cn12
InChI InChI=1S/C24H24FN7O2/c1-15-20-10-19(34-8-7-33-4)12-26-22(20)5-6-31(15)16(2)23-28-29-24-21(25)9-17(14-32(23)24)18-11-27-30(3)13-18/h5-6,9-14,16H,1,7-8H2,2-4H3
Molecular weight 461.20 Da
AlogP 0.0
HBond acceptors 9
HBond donors --
Atoms 58

References

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Expert Reviews

by SERP
(on 14 Dec 2020 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 14 Feb 2021 )
Cellular Use Rating
In Model Organisms
The receptor tyrosine kinase mesenchymal epithelial transition factor (MET) remains a target of interest primarily in the context of oncology where MET plays a critical role in cell growth, viability...
by SERP
(on 18 Feb 2021 )
Cellular Use Rating
In Model Organisms
Compound selectivity is outstanding for a kinase inhibitor with 0/402 kinases inhibited at 1 mM (PMID: 27196782). The plasma protein binding of AMG-337 is (relatively speaking) fairly low with unbound...
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