Home Protein Tyrosine Kinase c-Met inhibitor - RON inhibitor AMG-208 For research use only.

AMG-208

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

AMG-208 Chemical Structure

AMG-208 Chemical Structure

CAS: 1002304-34-8

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Biological Activity

Description AMG 208 is a highly selective dual c-Met and RON inhibitor with IC50 of 9 nM for c-Met.
Targets
c-Met [1]
9 nM
In vitro
In vitro AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, AMG-208 treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM. [1] Incubation of AMG-208 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 AMG-208 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] AMG-208 is identified to be a c-MET and RON dual selective inhibitor. [3]
In Vivo
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 AMG-208 (2 mg/kg i.v.) shows a bioavailability with AUC0→∞ of 2517 ng·h/mL and F of 43%, respectively. [1]
Animal Research Animal Models Male Sprague-Dawley rats
Dosages ≤2 mg/kg
Administration Administered via i.v. and p.o.
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

Chemical lnformation & Solubility

Molecular Weight 383.4 Formula

C22H17N5O2
CAS No. 1002304-34-8 SDF Download AMG-208 SDF
Smiles COC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5
Storage (From the date of receipt)

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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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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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.

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