AMG-208

SKU: orb1300928

Description

AMG-208 is a potent and selective small molecule inhibitor of the c-Met receptor tyrosine kinase, exhibiting an IC50 of 9 nM. It has been utilized in preclinical research to investigate c-Met-driven tumorigenesis in both cellular assays and animal models, supporting its role in oncology research.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1002304-34-8
• MW: 383.4
• Purity: 99.27% (May vary between batches)
• Formula: C₂₂H₁₇N₅O₂
• SMILES: COc1ccc2c(OCc3nnc4ccc(nn34)-c3ccccc3)ccnc2c1
• Target: c-Met/HGFR,Cytochromes P450
• Solubility: DMSO:2.5 mg/mL (6.52 mM)

Bioactivity

• Target IC50:
  c-Met:9 nM|CYP3A4:32 μM
• 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.
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• 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. 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. 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. AMG-208 is identified to be a c-MET and RON dual selective inhibitor.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, HGFR, Inhibitor, Cytochrome P450, CYPs, c-Met/HGFR, cMet, c-Met, cMet/HGFR, AMG 208, AMG208, AMG-208

Compound Identifiers

PubChem CID

24864821