Glumetinib (SCC244) - Moligand™, ≥98% , Inhibitor of MET proto-oncogene; receptor tyrosine kinase, CAS No.1642581-63-2, Inhibitor of MET proto-oncogene; receptor tyrosine kinase

CAS: 1642581-63-2 Cat. No.: G414110 Molecular Weight: 459.48

GRADE & PURITY Moligand™, ≥98%

Synonyms

UNII-7JTT036WGX | SCC244 | SC-C244 | AC-32584 | HY-116000 | SCC244; SC-C244; SCC 244 | 6-(1-Methyl-1H-pyrazol-4-yl)-1-((6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl)sulfonyl)-1H-pyrazolo[4,3-b]pyridine | 6-(1-methylpyrazol-4-yl)-1-[6-(1-methylpy

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

Information

Glumetinib (SCC244) Glumetinib (SCC244) is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. Glumetinib has greater than 2,400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, and TyrO3.

Targets

c-Met (Cell-free assay) 0.42 nM

In vitro

SCC244 strongly inhibits c-Met phosphorylation as well as AKT and ERK phosphorylation in EBC-1, MKN-45 cells harboring an amplified MET gene and U87MG cells responsive to HGF stimulation. SCC244 elicits selective and profound effects against c-Met-driven cancer cell proliferation. It inhibits c-Met-dependent neoplastic phenotypes of metastasis and angiogenesis.

In vivo

In xenografts of human tumor cell lines or non-small cell lung cancer and hepatocellular carcinoma patient-derived tumor tissue driven by MET aberration, SCC244 administration exhibits robust antitumor activity at the well-tolerated doses. In addition, the in vivo antitumor activity of SCC244 involves the inhibition of c-Met downstream signaling via a mechanism of combined antiproliferation and antiangiogenic effects.

Cell Research(from reference)

Cell lines：U87MG cells 

Concentrations：5, 10, 20 nM 

Incubation Time：2 h 

Specifications

Synonyms

UNII-7JTT036WGX | SCC244 | SC-C244 | AC-32584 | HY-116000 | SCC244; SC-C244; SCC 244 | 6-(1-Methyl-1H-pyrazol-4-yl)-1-((6-(1-methyl-1H-pyrazol-4-yl)imidazo[1, 2-a]pyridin-3-yl)sulfonyl)-1H-pyrazolo[4, 3-b]pyridine | 6-(1-methylpyrazol-4-yl)-1-[6-(1-methylpy

Specifications & Purity

Moligand™, ≥98%

Biochemical and Physiological Mechanisms

Glumetinib (SCC244) is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. Glumetinib has greater than 2, 400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homolo

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of MET proto-oncogene; receptor tyrosine kinase

Purity

≥98%

Product Properties

• ALogP: 1.725
• hba_count: 7
• Rotatable Bond: 4

Names and Identifiers

• Pubchem Sid: 504772834
• Pubchem Sid Url: https://pubchem.ncbi.nlm.nih.gov/substance/504772834
• Canonical Smiles: CN1C=C(C=N1)C2=CN3C(=NC=C3S(=O)(=O)N4C5=C(C=N4)N=CC(=C5)C6=CN(N=C6)C)C=C2
• IUPAC Name: 6-(1-methylpyrazol-4-yl)-1-[6-(1-methylpyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]sulfonylpyrazolo[4,3-b]pyridine
• InChIKey: RYBLECYFLJXEJX-UHFFFAOYSA-N
• INCHI: 1S/C21H17N9O2S/c1-27-11-16(7-24-27)14-3-4-20-23-10-21(29(20)13-14)33(31,32)30-19-5-15(6-22-18(19)9-26-30)17-8-25-28(2)12-17/h3-13H,1-2H3
• Isomeric SMILES: CN1C=C(C=N1)C2=CN3C(=NC=C3S(=O)(=O)N4C5=C(C=N4)N=CC(=C5)C6=CN(N=C6)C)C=C2
• Molecular Weight: 459.48
• Reaxy-Rn: 27905098
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27905098&ln=

Taxonomic Classification

Taxonomy Tree

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

• Kingdom: Organic compounds
• Superclass: Organoheterocyclic compounds
• Class: Pyridines and derivatives
• Subclass: Pyrazolylpyridines
• Intermediate Tree Nodes: Not available
• Direct Parent: Pyrazolylpyridines
• Alternative Parents: Pyrazolopyridines Imidazopyridines Imidazo[1,2-a]pyridines N-substituted imidazoles Sulfonyls Pyrazoles Organosulfonic acids and derivatives Heteroaromatic compounds Azacyclic compounds Organopnictogen compounds Organonitrogen compounds Organic oxides Hydrocarbon derivatives
• Molecular Framework: Aromatic heteropolycyclic compounds
• Substituents: 3-pyrazolylpyridine - Imidazo[1,2-a]pyridine - Pyrazolopyridine - Imidazopyridine - N-substituted imidazole - Heteroaromatic compound - Sulfonyl - Organosulfonic acid or derivatives - Organic sulfonic acid or derivatives - Pyrazole - Imidazole - Azole - Azacycle - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organosulfur compound - Organonitrogen compound - Aromatic heteropolycyclic compound
• Description: 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

Associated Targets(Human)

MET Tclin Hepatocyte growth factor receptor (0 Activities)

Discover Target: MET

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

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 11 mg/mL (23.94 mM); Water: Insoluble; Ethanol: Insoluble
• DMSO(mg / mL) Max Solubility: 11
• DMSO(mM) Max Solubility: 23.9401062070166
• Water(mg / mL) Max Solubility: ＜1
• Molecular Weight: 459.500 g/mol
• XLogP3: 1.900
• Hydrogen Bond Donor Count: 0
• Hydrogen Bond Acceptor Count: 7
• Rotatable Bond Count: 4
• Exact Mass: 459.123 Da
• Monoisotopic Mass: 459.123 Da
• Topological Polar Surface Area: 126.000 Ų
• Heavy Atom Count: 33
• Formal Charge: 0
• Complexity: 825.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 0
• 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