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AMG-337

Catalog No. T3209   CAS 1173699-31-4
Synonyms: AMG337

AMG-337 is an effective and highly specific ATP-competitive MET kinase inhibitor. In enzymatic assays, AMG-337(AMG337) inhibits MET kinase activity (IC50: < 5 nM).

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AMG-337 Chemical Structure
AMG-337, CAS 1173699-31-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 77.00
10 mg In stock $ 126.00
25 mg In stock $ 207.00
50 mg In stock $ 369.00
100 mg In stock $ 549.00
200 mg In stock $ 788.00
1 mL * 10 mM (in DMSO) In stock $ 78.00
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Purity: 99.9%
Purity: 99.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AMG-337 is an effective and highly specific ATP-competitive MET kinase inhibitor. In enzymatic assays, AMG-337(AMG337) inhibits MET kinase activity (IC50: < 5 nM).
Targets&IC50 MET kinase:< 5 nM
In vitro AMG 337 potently inhibits the enzymatic activity of WT MET and a subset of MET mutants found in papillary renal cell carcinoma. The inability of AMG 337 to inhibit the Y1230 and D1228 mutants is likely the result of a disruption of the inactive confirmation of the activation loop in the MET kinase domain. AMG 337 also inhibits cell based HGF-induced MET phosphorylation in PC3 cells with IC50 of 5 nM. AMG 337 inhibits proliferation in MET-dependent cancer cell lines. AMG 337 inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines resulting in profound effects on cell proliferation and survival[1].
In vivo AMG 337 exhibits impressive potency with >90% inhibition of Gab-1 phosphorylation at a dose of 0.75 mg/kg (32 nmol/L free-drug concentration). AMG 337 is well tolerated at continuously administered doses that corresponded with complete MET inhibition for 24 hours, suggesting that AMG 337 has the preClinicalal attributes required to test the role of MET in human cancer[1].
Cell Research To evaluate the effect of AMG 337 on viability, cells are seeded in 96-well plates at an optimal density to ensure proliferation throughout the duration of the experiments. Cells are treated for 72 hours with a 10-point, 3-fold, serial dilution of AMG 337 using a top concentration of 3 mmol/L. Viability is measured with the CellTiter-Glo Luminescent Cell Viability Assay.(Only for Reference)
Synonyms AMG337
Molecular Weight 463.46
Formula C23H22FN7O3
CAS No. 1173699-31-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 95 mg/mL (204.98 mM)

DMSO: 40 mg/mL

TargetMolReferences and Literature

1. Hughes PE, et al. Mol Cancer Ther. 2016, 15(7):1568-1579.

TargetMolCitations

1. Huang Y, Guo Y, Zhou Y, et al.Tivantinib alleviates inflammatory diseases by directly targeting NLRP3.iScience.2023

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Drug Library Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library NO PAINS Compound Library ReFRAME Related Library

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C-Met inhibitor D9 BMS817378 Glumetinib SAR125884 hydrochlorid (1116743-46-4(free base)) LMTK3-IN-1 Hepln-13 Altiratinib Caveolin-1 (82-101) amide (human, mouse, rat)

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Keywords

AMG-337 1173699-31-4 Tyrosine Kinase/Adaptors c-Met/HGFR Inhibitor anticancer MKN-45 cell proliferation SNU-5 cells AMG337 SNU-620 phosphorylation AMG 337 inhibit inhibitor

 

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