AMG-337

AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis[1][2].

Product Specifications

CAS Number

[1173699-31-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Caspase; c-Met/HGFR

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/AMG-337.html

Purity

99.40

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1C2=C(N=CC(OCCOC)=C2)C=CN1[C@@H](C3=NN=C4C(F)=CC(C5=CN(C)N=C5)=CN43)C

Molecular Formula

C23H22FN7O3

Molecular Weight

463.46

Precautions

H302, H315, H319, H335

References & Citations

[1]Hughes PE, et, al. In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models. Mol Cancer Ther. 2016 Jul;15 (7) :1568-79.|[2]Du Z, et, al. Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma. Mol Cancer Ther. 2016 Jun;15 (6) :1227-37.