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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
Vendors
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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

Vendors

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Expert Reviews

by SERP
(on 14 Dec 2020)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public 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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