Name: AMG 337
Brand: Selleck Chemicals
SKU: S8167
Rating: 5 (2 reviews)

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.73

Related Targets	EGFR VEGFR PDGFR FGFR Src MEK CSF-1R FLT3 HER2 c-Kit
Other c-Met Inhibitors	Tepotinib Dihexa SGX-523 PHA-665752 Foretinib SU11274 BMS-777607 JNJ-38877605 Tivantinib PF-04217903

Chemical Information, Storage & Stability

Molecular Weight	463.46	Formula	C₂₃H₂₂FN₇O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1173699-31-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C1=NN=C2N1C=C(C=C2F)C3=CN(N=C3)C)N4C=CC5=C(C4=O)C=C(C=N5)OCCOC

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (204.97 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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	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 this compound 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. It also inhibits cell based HGF-induced MET phosphorylation in PC3 cells with IC50 of 5nM. This compound inhibits proliferation in MET-dependent cancer cell lines. It inhibits signalling 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). This compound is well tolerated at continuously administered doses that corresponded with complete MET inhibition for 24 hours, suggesting that it has the preclinical attributes required to test the role of MET in human cancer.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27196782/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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AMG 337 c-Met inhibitor

Chemical Structure

Molecular Weight: 463.46