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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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