INCB28060 (Synonyms: Capmatinib, INC 280) |
Catalog No.GC17866 |
INCB28060 (INC280; INCB28060) es un potente inhibidor de la cinasa c-Met competitivo por ATP, activo por vÍa oral, selectivo y competitivo con ATP (IC50 = 0,13 nM). INCB28060 puede inhibir la fosforilaciÓn de c-MET, asÍ como los efectores posteriores de la vÍa c-MET, como ERK1/2, AKT, FAK, GAB1 y STAT3/5. INCB28060 inhibe de forma potente la proliferaciÓn y migraciÓn de células tumorales dependientes de c-MET e induce eficazmente la apoptosis. Actividad antitumoral. INCB28060 se metaboliza en gran medida por CYP3A4 y aldehÍdo oxidasa.
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Cas No.: 1029712-80-8
Sample solution is provided at 25 µL, 10mM.
INCB28060, also known as Capmatinib and INC280, is a novel and ATP-competitive inhibitor of c-Met with IC50 of 0.13 nM.
c-Met, also named as hepatocyte growth factor receptor (HGFR) is a receptor tyrosine kinase that is essential for embryonic development and would healing. In many tumor cells, this molecular is overexpressed or mutated and was found to play important roles in tumor cell proliferation, survival, invasion, metastasis and angiogenesis.
In vitro, INCB28060 treatment effectively inhibited activation of c-MET and signaling in cancer cells. As a result, INCB28060 blocked cell proliferation of varying cell lines such as SNU-5 and S114. The cell migration of U-87MG and H441 cells were also highly inhibited1.
The role of c-met was studied using this inhibitor in mouse model. Oral administration of INCB28060 leads to inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models. Therefore, INCB28060 has the therapeutic potential in cancer treatment 1.
Reference:
1. Liu X, Wang Q, Yang G, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011;17(22):7127-7138.
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