The store will not work correctly when cookies are disabled.
JavaScript seems to be disabled in your browser. For the best experience on our site, be sure to turn on Javascript in your browser.
Home Bioactive Small Molecules AMG 337 - 10mM in DMSO, high purity , CAS No.1173699-31-4, Inhibitor of CYP3A4;Inhibitor of MET proto-oncogene; receptor tyrosine kinase
AMG 337 - 10mM in DMSO, high purity , CAS No.1173699-31-4, Inhibitor of CYP3A4;Inhibitor of MET proto-oncogene; receptor tyrosine kinase
Basic Description Synonyms AMG-337 | 1173699-31-4 | AMG 337 | 08WG8S0L8D | AMG 337 [WHO-DD] | (r)-6-(1-(8-fluoro-6-(1-methyl-1h-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6h)-one | UNII-08WG8S0L8D | CHEMBL3785909 | 1,6-Naphthyridin-5(6H)-one, 6-( Specifications & Purity Moligand™, 10mM in DMSO Biochemical and Physiological Mechanisms AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM. Storage Temp Store at -80°C Shipped In Ice chest + Ice pads Grade Moligand™ Action Type INHIBITOR Mechanism of action Inhibitor of CYP3A4;Inhibitor of MET proto-oncogene; receptor tyrosine kinase Product Description Information
AMG 337 AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM.
Targets
MET receptor (Cell-free assay); MET(H1094R) (Cell-free assay); MET(M1250T) (Cell-free assay); MET(V1092I) (Cell-free assay) 1 nM; 1 nM ;4.7 nM; 21.5 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 5nM.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.
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 preclinical attributes required to test the role of MET in human cancer.
Cell Research(from reference)
Cell lines：Human cancer cell lines
Concentrations：serial dilution(a top concentration of 3 mmol/L.)
Incubation Time：72 h
Associated Targets(Human) Associated Targets(non-human) Mechanisms of Action Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References
Names and Identifiers IUPAC Name 6-[(1R)-1-[8-fluoro-6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl]-3-(2-methoxyethoxy)-1,6-naphthyridin-5-one INCHI 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 InChi Key DWHXUGDWKAIASB-CQSZACIVSA-N Canonical SMILES CC(C1=NN=C2N1C=C(C=C2F)C3=CN(N=C3)C)N4C=CC5=C(C4=O)C=C(C=N5)OCCOC Isomeric SMILES C[C@H](C1=NN=C2N1C=C(C=C2F)C3=CN(N=C3)C)N4C=CC5=C(C4=O)C=C(C=N5)OCCOC PubChem CID 44181686 Molecular Weight 463.46
Certificates（CoA,COO,BSE/TSE and Analysis Chart) Chemical and Physical Properties Molecular Weight 463.500 g/mol XLogP3 1.500 Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 8 Rotatable Bond Count 7 Exact Mass 463.177 Da Monoisotopic Mass 463.177 Da Topological Polar Surface Area 99.700 Ų Heavy Atom Count 34 Formal Charge 0 Complexity 760.000 Isotope Atom Count 0 Defined Atom Stereocenter Count 1 Undefined Atom Stereocenter Count 0 Defined Bond Stereocenter Count 0 Undefined Bond Stereocenter Count 0 The total count of all stereochemical bonds 0 Covalently-Bonded Unit Count 1
Safety and Hazards(GHS) Pictogram(s) GHS07 Signal Warning Hazard Statements H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H302: Harmful if swallowed
Precautionary Statements P305+P351+P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.
P280: Wear protective gloves/protective clothing/eye protection/face protection.
Solution Calculators Molarity Calculator Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator Determine the dilution needed to prepare a stock solution.
Reconstitution Calculator
