NPS-1034

  • 化学数据
CAS号 1221713-92-3 货号 BCP15998
中文名 NPS-1034
英文名 NPS-1034
中文别名
英文别名 NPS1034;NPS 1034;
分子式 C31H23F2N5O3 分子量 551.54
  • 用途
生物活性 NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.NPS-1034 is a novel MET inhibitor, which inhibits the activated MET receptor and its constitutively active mutants. NPS-1034, inhibits various constitutively active mutant forms of MET as well as HGF-activated wild-type MET. NPS-1034 inhibited the proliferation of cells expressing activated MET and promoted the regression of tumors formed from such cells in a mouse xenograft model through anti-angiogenic and pro-apoptotic actions. NPS-1034 also inhibited HGF-stimulated activation of MET signaling in the presence or absence of serum. Notably, NPS-1034 inhibited three MET variants that are resistant to the MET inhibitors SU11274, NVP-BVU972, and PHA665752.
信号通路 Angiogenesis/Protein Tyrosine Kinase 
靶 点 TAM Receptor 

结构式

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