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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 |
|---|
| Zurletrectinib
Zurletrectinib (ICP-723) is a potent tyrosine kinase inhibitor. Zurletrectinib serves as an antineoplastic agent. Zurletrectinib can used for research of TRK-mediated related diseases. |
| ABN401
ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. |
| (Z)-Semaxanib
(Z)-Semaxanib is a potent tyrosine kinase inhibitor. |
| MET kinase-IN-2
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. |
| BMS-817378
BMS-817378 is a potent and selective inhibitor of MET with IC50 of 1.7 nM. |
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Products are for research use only. Not for human use. We do not sell to patients.
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