BiochemProbe — Life Science Research Reagents

AMG337 free base · Synonyms: AMG-337 · AMG 337

AMG-337 is a potent, orally active, selective MET kinase inhibitor.

For research use only. Not for human or veterinary use.

Target c-Met/HGFR Caspase Apoptosis
Research area Cancer
Purity >98% Stock Inquire
Data Sheet SDS COA

AMG337 structure

CAS No.: 1173699-31-4

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
100 mg USD 470.00 BP-02480-100mg In stock Get quote
250 mg USD 930.00 BP-02480-250mg In stock Get quote
500 mg USD 1,480.00 BP-02480-500mg In stock Get quote
1 g USD 2,380.00 BP-02480-1g In stock Get quote
2 g USD 3,800.00 BP-02480-2g In stock Get quote
3 g USD 4,570.00 BP-02480-3g In stock Get quote
5 g USD 6,090.00 BP-02480-5g In stock Get quote

Need another size or custom synthesis? Request a quote.

Description

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 .

Biological activity

In Vitro AMG 337 (0-3 μM; 72 h) inhibits proliferation in MET-dependent cancer cell lines. AMG 337 (0-300 nM; 0-24 h; MKN-45, SNU-620, and SNU-5 cells) inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis. In Vivo AMG 337 (0-30 mg/kg; p.o.; daily, for 28 d) inhibits MET signaling in tumor xenografts and inhibits tumor growth in MET-dependent tumor xenograft models. AMG 337 (0-3 mg/kg; p.o.; once, for 3 or 24 h) is associated with increased necrosis in the MET-dependent SNU-620 tumor xenograft model.

Identifiers

SMILES
COCCOC1=CC2=C(C=CN(C(C)C3=NN=C4N3C=C(C=C4F)C3=CN(C)N=C3)C2=C)N=C1
InChIKey
WKIALOXOAZXGMG-UHFFFAOYSA-N

Specifications

MW (average)
461.4915
Formula
C24H24FN7O2
CAS No.
1173699-31-4
Physical state
Solid
Color
White to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[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.

Same target

Search c-Met/HGFR

Same research area

Search Cancer