Home Protein Tyrosine Kinase c-Met inhibitor AMG 337 For research use only.

AMG 337

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

AMG 337 Chemical Structure

AMG 337 Chemical Structure

CAS: 1173699-31-4

Selleck's AMG 337 has been cited by 2 publications

Purity & Quality Control

Batch: S816701 DMSO] 95 mg/mL] false] Ethanol] 95 mg/mL] false] Water] Insoluble] false Purity: 99.73%
99.73

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Biological Activity

Description AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor 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
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[1].
Cell Research Cell lines Human cancer cell lines
Concentrations serial dilution(a top concentration of 3 mmol/L.)
Incubation Time 72 h
Method

To evaluate the effect of AMG 337 on viability, cells are seeded in 96-well plates at an optimal density to ensure proliferation throughout the duration of the experiments. Cells are treated for 72 hours with a 10-point, 3-fold, serial dilution of AMG 337 using a top concentration of 3 mmol/L. Viability is measured with the CellTiter-Glo Luminescent Cell Viability Assay.
In Vivo
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[1].
Animal Research Animal Models Female CD1 nu/nu or athymic nude mice(Tumor xenograft models)
Dosages 0.1, 0.5, 0.75, 1, 2, or 3 mg/kg
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02096666 Completed Stomach Neoplasms Amgen April 15 2014 Phase 1|Phase 2
NCT02016534 Terminated Stomach Neoplasms Amgen February 2014 Phase 2
NCT01253707 Completed Advanced Malignancy|Advanced Solid Tumors|Cancer|Oncology|Oncology Patients|Tumors Amgen December 8 2010 Phase 1

Chemical lnformation & Solubility

Molecular Weight 463.46 Formula

C23H22FN7O3
CAS No. 1173699-31-4 SDF Download AMG 337 SDF
Smiles CC(C1=NN=C2N1C=C(C=C2F)C3=CN(N=C3)C)N4C=CC5=C(C4=O)C=C(C=N5)OCCOC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 95 mg/mL ( (204.97 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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