AMG 337 - Moligand™, ≥98% , Inhibitor of CYP3A4;Inhibitor of MET proto-oncogene; receptor tyrosine kinase, CAS No.1173699-31-4, Inhibitor of CYP3A4;Inhibitor of MET proto-oncogene; receptor tyrosine kinase

CAS: 1173699-31-4 Cat. No.: A413926 Formula: C₂₃H₂₂FN₇O₃ Peso molecolare: 463.46

GRADE & PURITY Moligand™, ≥98%

Synonyms

1,6-Naphthyridin-5(6H)-one, 6-((1R)-1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo(4,3-a)pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)- | AC-33036 | HY-18696 | SCHEMBL4304600 | UNII-08WG8S0L8D | NSC789223 | NSC-789223 | BDBM50157612 | GTPL8913 | AMG-33

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Panoramica

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 

Specifications

Sinonimi

1,6-Naphthyridin-5(6H)-one, 6-((1R)-1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo(4,3-a)pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)- | AC-33036 | HY-18696 | SCHEMBL4304600 | UNII-08WG8S0L8D | NSC789223 | NSC-789223 | BDBM50157612 | GTPL8913 | AMG-33

Specifiche e purezza

Moligand™, ≥98%

Meccanismi biochimici e fisiologici

AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM.

Condizioni di conservazione di stoccaggio

Store at -20°C

Spedito in

Ice chest + Ice pads

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

INHIBITOR

Meccanismo d'azione

Inhibitor of CYP3A4;Inhibitor of MET proto-oncogene; receptor tyrosine kinase

Purezza

≥98%

Nomi e identificatori

• Pubchem Sid: 504770296
• Pubchem Sid Url: https://pubchem.ncbi.nlm.nih.gov/substance/504770296
• Sorrisi canonici: CC(C1=NN=C2N1C=C(C=C2F)C3=CN(N=C3)C)N4C=CC5=C(C4=O)C=C(C=N5)OCCOC
• 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
• 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
• Isomeri 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
• Peso molecolare: 463.46
• Reaxy-Rn: 29325693
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29325693&ln=

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Organoheterocyclic compounds
    • Classe Pyridines and derivatives
      • Subclass Pyrazolylpyridines

• Kingdom: Organic compounds
• Superclass: Organoheterocyclic compounds
• Classe: Pyridines and derivatives
• Subclass: Pyrazolylpyridines
• Intermediate Tree Nodes: Not available
• Direct Parent: Pyrazolylpyridines
• Alternative Parents: Naphthyridines Triazolopyridines Pyridinones Alkyl aryl ethers Aryl fluorides Triazoles Pyrazoles Heteroaromatic compounds Lactams Dialkyl ethers Azacyclic compounds Organonitrogen compounds Organofluorides Organic oxides Hydrocarbon derivatives
• Molecular Framework: Aromatic heteropolycyclic compounds
• Substituents: 3-pyrazolylpyridine - Naphthyridine - Triazolopyridine - Alkyl aryl ether - Pyridinone - Aryl fluoride - Aryl halide - Azole - Heteroaromatic compound - 1,2,4-triazole - Triazole - Pyrazole - Lactam - Dialkyl ether - Ether - Azacycle - Organooxygen compound - Organic oxygen compound - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Organohalogen compound - Organofluoride - Organonitrogen compound - Aromatic heteropolycyclic compound
• Descrizione: This compound belongs to the class of organic compounds known as pyrazolylpyridines. These are compounds containing a pyrazolylpyridine skeleton, which consists of a pyrazole linked (not fused) to a pyridine by a bond.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Obiettivi associati (umani)

CYP3A4 Tclin Cytochrome P450 3A4 (1 Activities)

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor (3 Activities)

Discover Target: MET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor (10718 Activities)

Discover Target: MET

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Obiettivi associati (non umani)

Hdac6 Histone deacetylase 6 (222 Activities)

Discover Target: Hdac6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Canis familiaris (36305 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mus musculus (284745 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Rattus norvegicus (775804 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

rep Replicase polyprotein 1ab (378 Activities)

Discover Target: rep

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Plasma (328 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Liver microsome (341 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Meccanismi d'azione

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro DMSO: 95 mg/mL (204.97 mM); Ethanol: 95 mg/mL (204.97 mM); Water: Insoluble
• Peso molecolare: 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

Domande frequenti

What is the purity of this product?

This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1173699-31-4, the molecular formula is C23H22FN7O3, and the molecular weight is 463.46 g/mol. InChIKey DWHXUGDWKAIASB-CQSZACIVSA-N.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.