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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
中文名称
葡美替尼(SCC244), MET 原癌基因抑制剂
英文名称
Glumetinib (SCC244)
中文别名
-
英文别名
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号
1642581-63-2
分子式
C21H17N9O2S
分子量
459.48 g/mol
精确质量
-
PSA
126.000 Ų
Logp
1.725
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MedMol Glumetinib 98% 5mg

品牌:MedMol
货号:S88460-5mg
级别: -
货期:30天
已售 432 件
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