Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C30H29N5O5 |
| Molecular Weight | 539.5818 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C2C(OC3=CN=C(NC(=O)C4=C(C)N(CC(C)(C)O)N(C4=O)C5=CC=CC=C5)C=C3)=CC=NC2=C1
InChI
InChIKey=GLBZSOQDAOLMGC-UHFFFAOYSA-N
InChI=1S/C30H29N5O5/c1-19-27(29(37)35(20-8-6-5-7-9-20)34(19)18-30(2,3)38)28(36)33-26-13-11-22(17-32-26)40-25-14-15-31-24-16-21(39-4)10-12-23(24)25/h5-17,38H,18H2,1-4H3,(H,32,33,36)
| Molecular Formula | C30H29N5O5 |
| Molecular Weight | 539.5818 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/22320327
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/22320327
AMG-458 is a potent c-Met inhibitor. AMG-458 was found to significantly inhibit tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight. AMG-458 was advanced into preclinical safety studies in cancer in USA.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). | 2008 Jul 10 |
|
| Chemical reactivity of methoxy 4-o-aryl quinolines: identification of glutathione displacement products in vitro and in vivo. | 2008 Nov |
|
| Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation. | 2010 Jun |
Patents
Sample Use Guides
Mice: AMG-458 significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d.with no adverse effect on body weight. Administered orally
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:33:53 GMT 2023
by
admin
on
Sat Dec 16 08:33:53 GMT 2023
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| Record UNII |
4535RW5Y3A
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| Record Status |
Validated (UNII)
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