CAS 913376-83-7|AMG-458

Introduction：Basic information about CAS 913376-83-7|AMG-458, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. AMG-458 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	AMG-458
CAS Number	913376-83-7	Molecular Weight	539.582
Density	1.3±0.1 g/cm3	Boiling Point	/
Molecular Formula	C₃₀H₂₉N₅O₅	Melting Point	/
MSDS	/	Flash Point	/

Names

Name	1-(2-hydroxy-2-methylpropyl)-N-[5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide
Synonym	More Synonyms

AMG-458 BiologicalActivity

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].
Related Catalog	Research Areas >>CancerSignaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFR
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	[1]. Longbin Liu, et al. 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). J Med Chem. 2008 Jul 10;51(13):3688-91.

Chemical & Physical Properties

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
InChIKey	GLBZSOQDAOLMGC-UHFFFAOYSA-N
SMILES	COc1ccc2c(Oc3ccc(NC(=O)c4c(C)n(CC(C)(C)O)n(-c5ccccc5)c4=O)nc3)ccnc2c1
Storage condition	-20℃

Safety Information

Hazard Codes	N

Synonyms

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

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