BMS-986115
  • 化学数据
CAS号 1584647-27-7 货号 BCP49196
中文名 BMS-986115
英文名 BMS-986115
中文别名
英文别名 Notch inhibitor 1; BMS 986115; BMS986115;AL-102;AL 102;AL102;
分子式 C26H25F7N4O3 分子量 574.49
  • 用途
生物活性 BMS-986115 is an orally bioavailable, gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic activity. Upon administration, GS/pan-Notch inhibitor BMS 986115 binds to GS and blocks the proteolytic cleavage and release of the Notch intracellular domain (NICD), which would normally follow ligand binding to the extracellular domain of the Notch receptor. This prevents both the subsequent translocation of NICD to the nucleus to form a transcription factor complex and the expression of Notch-regulated genes. This results in the induction of apoptosis and the inhibition of growth of tumor cells that overexpress Notch. Overexpression of the Notch signaling pathway plays an important role in tumor cell proliferation and survival.
信号通路 Wnt/Stem Cell 
靶 点 Notch 

结构式

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