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Details

Stereochemistry ABSOLUTE
Molecular Formula C23H22FN7O3
Molecular Weight 463.4643
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMG-337

SMILES

COCCOC1=CC2=C(C=CN([C@H](C)C3=NN=C4N3C=C(C=C4F)C5=CN(C)N=C5)C2=O)N=C1

InChI

InChIKey=DWHXUGDWKAIASB-CQSZACIVSA-N
InChI=1S/C23H22FN7O3/c1-14(30-5-4-20-18(23(30)32)9-17(11-25-20)34-7-6-33-3)21-27-28-22-19(24)8-15(13-31(21)22)16-10-26-29(2)12-16/h4-5,8-14H,6-7H2,1-3H3/t14-/m1/s1

HIDE SMILES / InChI

Description

AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the cell surface enzyme called c-Met, which, when dysregulated, stimulates cancer cell scattering, invasion and protection from apoptosis. AMG 337, currently in Phase 2 development for the treatment of gastric and esophageal adenocarcinoma. In addition, recently was shown, that AMG 337 a promising and novel therapeutic strategy for targeting hepatocellular carcinomas with a dependence on HGF/MET signaling.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
4.01 μg/mL
300 mg single, oral
AMG-337 plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
47.8 μg × h/mL
300 mg single, oral
AMG-337 plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
7 h
300 mg single, oral
AMG-337 plasma
Homo sapiens

PubMed

Sample Use Guides

In Vivo Use Guide
150 mg, 200 mg and 300 mg orally daily. Additional 150 mg and 200 mg orally twice daily.
Route of Administration: Oral
In Vitro Use Guide
Unknown