GLUMETINIB (SCC244)
Glumetinib
CAS: 1642581-63-2
Molecular Formula: C21H17N9O2S
GLUMETINIB (SCC244) - Names and Identifiers
GLUMETINIB (SCC244) - Physico-chemical Properties
| Molecular Formula | C21H17N9O2S |
| Molar Mass | 459.48 |
| Density | 1.61±0.1 g/cm3(Predicted) |
| Solubility | Soluble in DMSO |
| Appearance | solid |
| Color | Beige |
| pKa | 0.09±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Use | Glumetinib, also known as SCC244, is a novel, potent and highly selective inhibitor of c-Met in MET-dependent cancer models. SCC244 showed subnanomolar potency against c-Met kinase activity and high selectivity versus 312 other tested protein kinases, making it one of the most selective c-Met inhibitors described to date. Moreover, this inhibitor profoundly and specifically inhibits c-Met signal transduction and thereby suppresses the c-Met-dependent neoplastic phenotype of tumor and endothelial cells. |
| Target | IC50: 0.42 nM (c-Met kinase) |
| In vitro study | SCC244 strongly inhibited c-Met, AKT, and ERK phosphorylation in EBC-1 with amplified MET gene, in MKN-45 cells, and in HGF-stimulated U87MG cells. SCC244 can have a selective and profound effect on c-Met-driven cancer cell proliferation. SCC244 inhibits c-Met-dependent tumor phenotypes such as metastasis and angiogenesis. |
| In vivo study | In xenograft models of human-derived tumor cells or non-small cell lung cancer, or in tumor tissues of liver cancer patients driven by MET abnormalities, SCC244 has potent anti-tumor activity at various tolerated doses. SCC244 can c-MET downstream pathways through antiproliferative and antiangiogenic inhibition. |
GLUMETINIB (SCC244) - Reference
| Reference Show more | [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. |
GLUMETINIB (SCC244) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.176 ml | 10.882 ml | 21.764 ml |
| 5 mM | 0.435 ml | 2.176 ml | 4.353 ml |
| 10 mM | 0.218 ml | 1.088 ml | 2.176 ml |
| 5 mM | 0.044 ml | 0.218 ml | 0.435 ml |
Last Update：2024-01-02 23:10:35
GLUMETINIB (SCC244) - Cell Experiment
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.
Last Update：2023-08-16 21:32:38
GLUMETINIB (SCC244) - Animal Experiment
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%.
Last Update：2023-08-16 21:32:38
Supplier List
Spot supply
Product Name: Glumetinib Visit Supplier Webpage Request for quotationCAS: 1642581-63-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: Glumetinib Visit Supplier Webpage Request for quotationCAS: 1642581-63-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History