AMG-208

SKU: orb1227179

Description

AMG-208 is a potent, small-molecule c-Met inhibitor with IC50 of 5.2 nM against wt MET kinase, also inhibits VEGFR2 with IC50 of 112 nM; inhibits HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM, suppresses proliferation and induces apoptosis in human tumor xenograft models.Prostate Cancer Phase 2 Clinical(In Vitro):AMG-208 (compound 4) treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM.Pre-incubation of AMG-208 (compound 1) 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.(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.

Key Properties

• CAS Number: 1002304-34-8
• MW: 383.4027
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₇N₅O₂
• SMILES: COC1=CC=C2C(OCC3=NN=C4C=CC(C5=CC=CC=C5)=NN43)=CC=NC2=C1
• Target: c-Met/HGFR
• Solubility: DMSO: < 1 mg/mL

Bioactivity

• 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.
• In Vitro:
  AMG-208 (compound 4) treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM. Pre-incubation of AMG-208 (compound 1) 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AMG208 | AMG 208

Quick Database Links

Gene Symbol

c-Met/HGFR