INCB28060 (Synonyms: Capmatinib, INC 280) |
カタログ番号GC17866 |
INCB28060 (INC280; INCB28060) は、強力な経口活性、選択的、ATP 競合的 c-Met キナーゼ阻害剤です (IC50=0.13 nM)。 INCB28060 は、c-MET のリン酸化だけでなく、ERK1/2、AKT、FAK、GAB1、STAT3/5 などの c-MET 経路下流エフェクターのリン酸化も阻害できます。 INCB28060 は、c-MET 依存性腫瘍細胞の増殖と移動を強力に阻害し、効果的にアポトーシスを誘導します。抗腫瘍活性。 INCB28060 は、CYP3A4 とアルデヒドオキシダーゼによって大部分が代謝されます。
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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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