AMG-458
Modify Date: 2024-01-02 08:46:08
AMG-458 structure
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Common Name | AMG-458 | ||
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| CAS Number | 913376-83-7 | Molecular Weight | 539.582 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C30H29N5O5 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of AMG-458AMG-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[1]. |
| Name | 1-(2-hydroxy-2-methylpropyl)-N-[5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide |
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| Synonym | More Synonyms |
| Description | 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[1]. |
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| Related Catalog | |
| Target |
human c-Met:1.2 nM (Ki) mouse c-Met:2.0 nM (Ki) V1092I:1.1 nM (Ki) D1228H:2.2 nM (Ki) M1250T:4.1 nM (Ki) H1094R:0.5 nM (Ki) Y1230H:4.5 nM (Ki) VEGDR2:4100 nM (Ki) |
| In Vivo | AMG-458 (orally, 30, 100 mg/kg) significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight[1]. Animal Model: NIH-3T3/TPR-Met model and U-87 MG human glioblastoma xenograft model[1]. Dosage: 10, 30, 100 mg/kg. Administration: Orally q.d. or b.i.d. Result: With an ED50 of ∼12 mg/kg and an ED90 of ∼ 34 mg/kg in NIH-3T3/TPR-Met model. With an ED50 of ∼16 mg/kg and an ED90 of ∼ 59 mg/kg in U-87 MG human glioblastoma xenograft model. Significantly inhibited tumor growth at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d. without adverse effect on body weight. Animal Model: Balb/c mouse and SD rat[1]. Dosage: 1 mg/kg (Pharmacokinetic Analysis). Administration: IV dose: 1 mg/kg (20% Captisol with pH adjusted to 3.5 using methanesulfonic acid). Result: Exhibited CL ((L/h)/kg) values of 0.16 and 0.73, Vss (L/kg) values of 0.31 and 0.62, t1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C30H29N5O5 |
| Molecular Weight | 539.582 |
| Exact Mass | 539.216858 |
| PSA | 123.99000 |
| LogP | 3.02 |
| Index of Refraction | 1.672 |
| Storage condition | -20℃ |
| Hazard Codes | N |
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| 1-(2-Hydroxy-2-methylpropyl)-N-{5-[(7-methoxy-4-quinolinyl)oxy]-2-pyridinyl}-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide |
| cc-602 |
| AMG458 |
| AMG-458,AMG458 |
| Substituted Pyrazolone,17 |
| UNII-4535RW5Y3A |