AMG-337

SKU: orb1304422

Description

AMG-337 is a potent and selective ATP-competitive inhibitor of the MET kinase, demonstrating an IC50 of less than 5 nM in enzymatic assays. It is a valuable research tool for investigating MET-driven pathologies in both cellular and animal models, with applications in oncology and cancer research.

Research Area

Cell Biology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 1173699-31-4
• MW: 463.46
• Purity: 99.26% (May vary between batches)
• Formula: C₂₃H₂₂FN₇O₃
• SMILES: COCCOc1cnc2ccn([C@H](C)c3nnc4c(F)cc(cn34)-c3cnn(C)c3)c(=O)c2c1
• Target: Caspase,c-Met/HGFR,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.32 mM);Ethanol:95 mg/mL (204.98 mM);DMSO:50 mg/mL (107.88 mM)

Bioactivity

• Target IC50:
  MET:< 5 nM
• In Vivo:
  AMG 337 exhibits impressive potency with >90% inhibition of Gab-1 phosphorylation at a dose of 0.75 mg/kg (32 nmol/L free-drug concentration). AMG 337 is well tolerated at continuously administered doses that corresponded with complete MET inhibition for 24 hours, suggesting that AMG 337 has the preClinicalal attributes required to test the role of MET in human cancer.
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• In Vitro:
  AMG 337 potently inhibits the enzymatic activity of WT MET and a subset of MET mutants found in papillary renal cell carcinoma. The inability of AMG 337 to inhibit the Y1230 and D1228 mutants is likely the result of a disruption of the inactive confirmation of the activation loop in the MET kinase domain. AMG 337 also inhibits cell based HGF-induced MET phosphorylation in PC3 cells with IC50 of 5 nM. AMG 337 inhibits proliferation in MET-dependent cancer cell lines. AMG 337 inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines resulting in profound effects on cell proliferation and survival.
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• Cell Research:
  To evaluate the effect of AMG 337 on viability, cells are seeded in 96-well plates at an optimal density to ensure proliferation throughout the duration of the experiments. Cells are treated for 72 hours with a 10-point, 3-fold, serial dilution of AMG 337 using a top concentration of 3 mmol/L. Viability is measured with the CellTiter-Glo Luminescent Cell Viability Assay.(Only for Reference)
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Storage & Handling

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

Alternative Names

anticancer, AMG 337, AMG337, AMG-337, cell proliferation, cMet, c-Met, c-Met/HGFR, cMet/HGFR, inhibit, Inhibitor, MKN-45, Met, Met(H1094R), Met(M1250T), Met(V1092I), Met(Y1230H), HGFR, phosphorylation, SNU-5 cells, SNU-620

Compound Identifiers

PubChem CID

44181686