AMG-337

Modify Date: 2024-01-11 12:06:00

AMG-337 Structure
AMG-337 structure
Common Name AMG-337
CAS Number 1173699-31-4 Molecular Weight 463.464
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C23H22FN7O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AMG-337


AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.IC50 value: < 5nM [1]Target: METin vitro: AMG-337 demonstrates exquisite selectivity for MET when profiled against a diverse panel of over 400 protein and lipid kinases in a competitive binding assay. In cellular assays, AMG 337 inhibits HGF-dependent MET phosphorylation with an IC50 of < 10 nM. [1] AMG 337 is a selective inhibitor of Met, which inhibits multiple mechanisms of Met activation. [2]in vivo: AMG-337 demonstrates robust activity in MET-dependent cancer models. Oral administration of AMG 337 results in robust dose-dependent anti-tumor efficacy in MET amplified gastric cancer xenograft models, with inhibition of tumor growth consistent with the pharmacodynamic modulation of MET signaling.[1]

 Names

Name amg-337
Synonym More Synonyms

 AMG-337 Biological Activity

Description AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.IC50 value: < 5nM [1]Target: METin vitro: AMG-337 demonstrates exquisite selectivity for MET when profiled against a diverse panel of over 400 protein and lipid kinases in a competitive binding assay. In cellular assays, AMG 337 inhibits HGF-dependent MET phosphorylation with an IC50 of < 10 nM. [1] AMG 337 is a selective inhibitor of Met, which inhibits multiple mechanisms of Met activation. [2]in vivo: AMG-337 demonstrates robust activity in MET-dependent cancer models. Oral administration of AMG 337 results in robust dose-dependent anti-tumor efficacy in MET amplified gastric cancer xenograft models, with inhibition of tumor growth consistent with the pharmacodynamic modulation of MET signaling.[1]
Related Catalog
References

[1]. Paul E. Hughes, et al. AMG 337, a novel, potent and selective MET kinase inhibitor, has robust growth inhibitory activity in MET-dependent cancer models. Cancer Res October 1, 2014 74; 728

[2]. Cecchi F, et al. Targeting the HGF/Met signaling pathway in cancer therapy. Expert Opin Ther Targets. 2012 Jun;16(6):553-572.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C23H22FN7O3
Molecular Weight 463.464
Exact Mass 463.176819
PSA 101.36000
LogP 1.42
Index of Refraction 1.689
Storage condition -20℃

 Safety Information

Hazard Codes N

 Synonyms

6-{(1R)-1-[8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one
AMG337
(R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one
1,6-Naphthyridin-5(6H)-one, 6-[(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-a]pyridin-3-yl]ethyl]-3-(2-methoxyethoxy)-
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