AMG-208

Catalog No.S1316

AMG-208 Chemical Structure

Molecular Weight(MW): 383.4

AMG 208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1.

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Biological Activity

Description AMG 208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1.
Targets
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, 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 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]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Male Sprague-Dawley rats
  • Formulation: AMG-208 is dissolved in DMSO.
  • Dosages: ≤2 mg/kg
  • Administration: Administered via i.v. and p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.25 mg/mL (0.65 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 383.4
Formula

C22H17N5O2

CAS No. 1002304-34-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02420587 Withdrawn Prostate Cancer M.D. Anderson Cancer Center|Amgen October 2014 Phase 2
NCT00813384 Completed Cancer|Oncology|Tumors|Advanced Malignancy|Advanced Solid Tumors|Oncology Patients Amgen December 2008 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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c-Met Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID