1173699-31-4

Name	AMG-337
Synonyms	CS-1559 AMG 337 AMG-337 (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 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 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)-
CAS	1173699-31-4

Molecular Formula	C23H22FN7O3
Molar Mass	463.46
Density	1.44±0.1 g/cm3(Predicted)
Solubility	DMSO: ≥ 30 mg/mL
Appearance	Solid
Color	Pale Yellow
pKa	2.10±0.20(Predicted)
Storage Condition	Refrigerator, under inert atmosphere
In vitro study	AMG 337 potently inhibits the enzymatic activity of wild-type MET as well as some MET mutants in papillary cell carcinoma. The inability of AMG 337 to inhibit the Y1230 and D1228 MET mutants may be due to the disruption of the inactive conformation of the activation loop of the MET kinase region. AMG 337 also inhibited HGF-induced MET phosphorylation in PC3 cells with an IC50 of 5 nM. AMG 337 inhibits the proliferation of MET-dependent cancer cells, and plays a role in cell proliferation and survival through PI3K and MAPK signaling pathways in MET-signaling amplified gastric cancer cells.
In vivo study	AMG 337(0.75 mg/kg) inhibited phosphorylation of Gab-1 by more than 90%. It was well tolerated when MET was completely inhibited by 24 hours of continuous administration. Thus, AMG 337 has the clinical attribute of examining the role of MET in human cancer.

Last Update：2024-01-02 23:10:35

biological activity	AMG 337 is an oral, ATP competitive, highly selective Met (c-Met) receptor inhibitor. IC50 is 1 nM.
target	TargetValue MET receptor (cell-free assay) 1 nm MET (h1094r) (cell-free assay) 1 nm MET (m1250t) (cell-free assay) 4.7 nm MET (v1092i) (cell-free assay) 21.5 nm
Target	Value
MET receptor (Cell-free assay)	1 nM
MET(H1094R) (Cell-free assay)	1 nM
MET(M1250T) (Cell-free assay)	4.7 nM
MET(V1092I) (Cell-free assay)	21.5 nM
In vitro study	AMG 337 effectively inhibit wild-type MET and the enzyme activity of some MET mutants in papillary cell carcinoma. The inability of AMG 337 to inhibit Y1230 and D1228 MET mutants may be due to the destruction of the inactive conformation of the activation loop of the MET kinase region. AMG 337 also inhibited MET phosphorylation induced by HGF in PC3 cells with an IC50 of 5 nM. AMG 337 inhibits the proliferation of MET-dependent cancer cells and plays a role in cell proliferation and survival through PI3K and MAPK signaling pathways in MET-amplified gastric cancer cells.
in vivo studies	AMG 337(0.75 mg/kg) can inhibit the phosphorylation of Gab-1 greater than 90%. It was well tolerated with complete inhibition of MET after 24 hours of continuous administration. Therefore, AMG 337 has the clinical attribute of testing MET effect in human cancer.

Last Update：2024-04-09 21:04:16

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Product Name: AMG-337 Visit Supplier Webpage Request for quotation
CAS: 1173699-31-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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1173699-31-4

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