INCB28060 (Synonyms: Capmatinib, INC 280) |
Catalog No.GC17866 |
INCB28060(INC280, INCB28060)은 강력한 경구 활성, 선택적 ATP 경쟁 c-Met 키나제 억제제(IC50=0.13nM)입니다. INCB28060은 c-MET 및 ERK1/2, AKT, FAK, GAB1 및 STAT3/5와 같은 c-MET 경로 다운스트림 이펙터의 인산화를 억제할 수 있습니다. INCB28060은 c-MET 의존성 종양 세포 증식 및 이동을 강력하게 억제하고 효과적으로 세포 사멸을 유도합니다. 항종양 활성. INCB28060은 CYP3A4와 알데히드 산화효소에 의해 크게 대사됩니다.
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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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