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Glumetinib

Catalog No. T5414 CAS 1642581-63-2

Synonyms: SCC244

Glumetinib (SCC244) (SCC 244) is a novel potent and selective inhibitor of c-Met kinase (IC50: 0.42 nM).

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Glumetinib, CAS 1642581-63-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 50.00
5 mg	In stock	$ 113.00
10 mg	In stock	$ 173.00
25 mg	In stock	$ 292.00
50 mg	In stock	$ 437.00
100 mg	In stock	$ 646.00
1 mL * 10 mM (in DMSO)	In stock	$ 122.00

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Purity: 100%

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Description	Glumetinib (SCC244) (SCC 244) is a novel potent and selective inhibitor of c-Met kinase (IC50: 0.42 nM).
Targets&IC50	c-Met:0.42 nM (cell free)
In vitro	SCC244 exhibited high potency (IC50: 0.42 nM) against purified c-Met kinase activity using ELISA kinase assay. SCC244 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. SCC244 strongly suppressed HGF-induced NCI-H441 cell motility and invasion in a dose-dependent manner and was sufficient to block the movement of most cells at a dose of 10 nmol/L.
In vivo	In the MKN-45 model, SCC244 significantly inhibited tumor growth with inhibitory rates of 99.3%, 88.6%, and 63.6% at doses of 10, 5, and 2.5 mg/kg, respectively. In addition, tumor stasis was observed following a 21-day treatment with 5 and 10 mg/kg SCC244. Similar results were obtained in the SNU-5 model treated with SCC244, and tumor regression was observed in the high dose group. In the EBC-1 study, all mice receiving SCC244 exhibited a greater than 66.0% decrease in tumor mass, and in both the 10 and 5 mg/kg treatment groups, 1 of 6 mice exhibited no evidence of a tumor. Moreover, in all the tested models, the efficacy of SCC244 at 10 mg/kg is comparable with that of INCB28060 at 15 mg/kg and crizotinib at 50 mg/kg.
Kinase Assay	Met, Ron, Axl, TyrO3, and Mer kinases activity were assessed using both ELISA and radiometric protein kinase assays. The kinase selectivity profile of SCC244 (1 μmol/L) was screened against a panel of other 308 recombinant kinases using radiometric protein kinase assays was also performed according to the manufacturer's specifications.
Cell Research	Cells were seeded in 96-well plates at a low density in growth media. The next day, appropriate controls or designated concentrations of compounds were added to each well, and the cells were incubated for 72 hours. HUVECs (passage 3) were seeded in 96-well plates in growth media overnight and transferred to serum-free media for 24 hours. The following day, appropriate controls or designated concentrations of compounds were added to each well, and HGF was added to designated wells at 100 ng/mL. The cells were incubated for 48 hours. Finally, cell proliferation was determined using a sulforhodamine B assay, a thiazolyl blue tetrazolium bromide assay or a cell counting kit (CCK-8) assay.
Animal Research	To assess the pharmacodynamics of SCC244 in tumors, mice bearing established xenograft tumors were treated with a single dose of the compound at 10 or 2.5 mg/kg, and tumors were harvested at several time points. At a designated time following administration, mice were humanely euthanized, and their tumors were resected. The tumors were snap-frozen in liquid nitrogen and then homogenized in 500 μL of protein extraction solution (radioimmunoprecipitation assay, RIPA). The tumor extracts were then subjected to Western blot analysis. The individual bands of phospho-c-Met, phospho-AKT, and phospho-ERK were scanned and quantified using Gel Pro Analyzer software. The relative tyrosine phosphorylation of each sample at the indicated time points was then calculated, with the average value of vehicle-treated sample used as 100%.

Synonyms	SCC244
Molecular Weight	459.48
Formula	C21H17N9O2S
CAS No.	1642581-63-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.59 mg/mL (10 mM), Sonification is recommended

References and Literature

1. Ai J, et al. Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models. Mol Cancer Ther. 2018 Apr;17(4):751-762.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Highly Selective Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Glumetinib 1642581-63-2 Tyrosine Kinase/Adaptors c-Met/HGFR proliferation tumor cancer SCC244 bioavailable oral HCC inhibit SCC-244 ATP-competitive cell NSCLC Inhibitor SCC 244 inhibitor

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