Glumetinib (SCC244)

Catalog No.S8676

Glumetinib (SCC244) Chemical Structure

Molecular Weight(MW): 459.48

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.

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Biological Activity

Description 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 [1]
(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[1].

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].

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female nude mice with xenograft tumors
  • Formulation: --
  • Dosages: 10 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 11 mg/mL (23.94 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 459.48
Formula

C21H17N9O2S

CAS No. 1642581-63-2
Storage powder
in solvent
Synonyms N/A

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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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c-Met Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID