Information Glumetinib (SCC244) 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 (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. 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. Cell Research(from reference) Cell lines：U87MG cells Concentrations：5, 10, 20 nM Incubation Time：2 h
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Glumetinib (SCC244)
CAS number：1642581-63-2 molecular formula：C21H17N9O2S
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| Chinese alias | - | ||
| English alias | UNII-7JTT036WGX | SCC244 | SC-C244 | AC-32584 | HY-116000 | SCC244; SC-C244; SCC 244 | 6-(1-Methyl-1H-pyrazol-4-yl)-1-((6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl)sulfonyl)-1H-pyrazolo[4,3-b]pyridine | 6-(1-methylpyrazol-4-yl)-1-[6-(1-methylpy | ||
| CAS number | 1642581-63-2 | molecular formula | C21H17N9O2S |
| molecular weight | 459.48 g/mol | Exact mass | - |
| PSA | 126.000 Ų | logp | 1.725 |
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