Home Protein Tyrosine Kinase c-Met inhibitor - RON inhibitor Glumetinib For research use only.

Glumetinib

Synonyms: SCC244

Glumetinib 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.

Glumetinib Chemical Structure

Glumetinib Chemical Structure

CAS No. 1642581-63-2

Purity & Quality Control

Glumetinib Related Products

Signaling Pathway

c-Met Signaling Pathways

c-Met Signaling Pathway

Biological Activity

Description Glumetinib 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 [1]
(Cell-free assay)
0.42 nM
In vitro
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[1].
Cell Research Cell lines U87MG cells
Concentrations 5, 10, 20 nM
Incubation Time 2 h
Method

U87MG cells are serum-deprived for 24 hours prior to 2-hour treatment with SCC244 and then stimulated with HGF for 15 minutes. Next, the cells are lysed and subjected to Western blot analysis.
In Vivo
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[1].
Animal Research Animal Models Female nude mice with xenograft tumors
Dosages 10 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04270591 Recruiting
C-Met Exon 14 Mutation
Haihe Biopharma Co. Ltd.
 July 15 2019 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 459.48 Formula

C21H17N9O2S
CAS No. 1642581-63-2 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 11 mg/mL ( (23.94 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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