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AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively.
AMG-458 (30, 100 mg/kg; orally) significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight.
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Source | Int J Radiat Oncol Biol Phys (2012). Figure 2. AMG-458 |
| Method | Clonogenic assay | |
| Cell Lines | A549 and H441 lung cancer cells | |
| Concentrations | 5 μmol/L | |
| Incubation Time | 2 h | |
| Results | Treatment of H441 cells with 5-mmol/L AMG-458 before radiation caused a significant survival curve shift in H441 cells relative to DMSO-treated cells |
| Molecular Weight | 539.58 |
| Formula | C30H29N5O5 |
| CAS Number | 913376-83-7 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL (ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related c-Met Products |
|---|
| AMG-208
AMG-208 is a potent small molecular inhibitor c-Met with an IC50 of 9.3 nM. AMG-208 is also a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity. |
| BMS-777607
BMS-777607 is a selective and potent small-molecule met kinase inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively. |
| BMS 794833
BMS-794833 is a potent ATP competitive Met/VEGFR-2 kinase inhibitor. |
| XL-184
Cabozantinib (XL184, BMS-907351) is a small molecule inhibits multiple receptor tyrosine kinases, specifically MET and VEGFR2 with IC50 values of 0.035 and 1.8 nM for VEGFR2 and Met respectively. |
| Foretinib
Foretinib (XL880, GSK1363089) is a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2 (VEGFR2) with IC50 value of 0.4 nM for c-MET. |
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