中文名：葡美替尼（SCC244）
英文名：Glumetinib (SCC244)
纯度：Moligand™，≥98%
货号：G414110
Cas号：1642581-63-2
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
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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关键字： 谷美替尼;UNII-7JTT036WGX ; SCC244 ; SC-C244
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