Home Protein Tyrosine Kinase c-Met inhibitor - RON inhibitor AMG-208

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AMG-208 c-Met inhibitor

Cat.No.S1316

AMG 208 is a highly selective dual c-Met and RON inhibitor with IC50 of 9 nM for c-Met.
AMG-208 c-Met inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 383.4

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Chemical Information, Storage & Stability

Molecular Weight 383.4 Formula

C22H17N5O2

 Storage (From the date of receipt)
CAS No. 1002304-34-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5

Solubility

In vitro
Batch:

4-Methylpyridine : 10 mg/mL

DMSO : 0.4 mg/mL ( (1.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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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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Mechanism of Action

Targets/IC50/Ki
c-Met [1]
9 nM
In vitro
AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, this compound treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM. [1] Incubation of this chemical with rat and human liver microsomes in the presence of NADPH qualitatively yields C6-phenylarene oxidation products as the major metabolites. [1] Pre-incubation of this compound with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation. [2] This compound is identified to be a c-MET and RON dual selective inhibitor. [3]
In vivo
In male Sprague−Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour, while this compound (2 mg/kg i.v.) shows a bioavailability with AUC0→∞ of 2517 ng·h/mL and F of 43%, respectively. [1]
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00813384 Completed
Cancer|Oncology|Tumors|Advanced Malignancy|Advanced Solid Tumors|Oncology Patients
Amgen
 December 2008 Phase 1

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