[CAS NO. 1173699-31-4] AMG 337

Name: AMG 337
Brand: Arctom Scientific
SKU: SLK-S8167

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PRODUCTS SPECIFICATIONS [1173699-31-4]

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Catalog

SLK-S8167

Brand

Selleck

CAS

1173699-31-4

DESCRIPTION [1173699-31-4]

Overview

MDL	-
Molecular Weight	463.46
Molecular Formula	C23H22FN7O3
SMILES	O=C1C2=C(N=CC(OCCOC)=C2)C=CN1[C@@H](C3=NN=C4C(F)=CC(C5=CN(C)N=C5)=CN43)C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.1577 mL	10.7884 mL	21.5768 mL
5 mM	0.4315 mL	2.1577 mL	4.3154 mL
10 mM	0.2158 mL	1.0788 mL	2.1577 mL
50 mM	0.0432 mL	0.2158 mL	0.4315 mL

Description

AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the with an IC50 of 1 nM.

Targets

MET receptor ^[1] (Cell-free assay)	MET(H1094R) ^[1] (Cell-free assay)	MET(M1250T) ^[1] (Cell-free assay)	MET(V1092I) ^[1] (Cell-free assay)
1 nM	1 nM	4.7 nM	21.5 nM

In vitro

AMG 337 potently inhibits the enzymatic activity of WT MET and a subset of MET mutants found in papillary renal cell carcinoma. The inability of AMG 337 to inhibit the Y1230 and D1228 mutants is likely the result of a disruption of the inactive confirmation of the activation loop in the MET kinase domain. AMG 337 also inhibits cell based HGF-induced MET phosphorylation in PC3 cells with IC50 of 5nM. AMG 337 inhibits proliferation in MET-dependent cancer cell lines. AMG 337 inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines resulting in profound effects on cell proliferation and survival.

In vivo

AMG 337 exhibits impressive potency with >90% inhibition of Gab-1 phosphorylation at a dose of 0.75 mg/kg (32 nmol/L free-drug concentration). AMG 337 is well tolerated at continuously administered doses that corresponded with complete MET inhibition for 24 hours, suggesting that AMG 337 has the preclinical attributes required to test the role of MET in human cancer.

References

[1] Hughes PE, et al. Mol Cancer Ther. 2016, 15(7):1568-1579.