Glumetinib

Catalog No.S8676 Batch:S867601

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Technical Data

Formula

C21H17N9O2S
Molecular Weight 459.48 CAS No. 1642581-63-2
Solubility (25°C)* In vitro DMSO 11 mg/mL (23.94 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    Female nude mice with xenograft tumors

  • Dosages

    10 mg/kg

  • Administration

    oral

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.