LGK974，L974-002/010/050

产品信息

Wnt通路调节动物发育过程中的多个重要环节，例如细胞增殖、细胞迁徙及细胞分化。Wnt信号通路调控剂通过自分泌或旁分泌作用与位于细胞膜上的受体相结合，激活细胞内信号通路调节靶基因的表达，对细胞的增殖、分化、迁移、极性化和凋亡起到重要作用

LGK974 is a potent and specificinhibitor of O-acyltransferase Porcupine (Porcn) that acylates Wnt proteins required for their biological activities. The structure of LGK974 was recently published and found not only more potent than the IWP-1, 2, 3 or IWP-4 Porcn inhibitors, but LGK974 is also suitable for in-vivo studies and is currently in Phase I clinical trials to treat cancers.

Purity:
Greater than 99% as determined by LC/MSanalysis.

Biological Activity:
Biological activity has been determined. In a co-culture assay measuring the activation of the TCF reporter gene by Wnt3a-secreting cells, this compound gives IC50 of 0.2to 0.6nM. Pan and colleagues reported antitumor activity of LGK974 in xenograft models of human head and neck as well as pancreatic tumors when dosed at 1 to 10 mg/kg orally.

重庆市华雅干细胞技术有限公司