葡美替x（SCC244）

中文名：葡美替x（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：超低温冰袋运输

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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