Wnt通路調(diào)節(jié)動(dòng)物發(fā)育過程中的多個(gè)重要環(huán)節(jié)，例如細(xì)胞增殖、細(xì)胞遷徙及細(xì)胞分化。Wnt信號通路調(diào)控劑通過自分泌或旁分泌作用與位于細(xì)胞膜上的受體相結(jié)合，激活細(xì)胞內(nèi)信號通路調(diào)節(jié)靶基因的表達(dá)，對細(xì)胞的增殖、分化、遷移、極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.

重慶市華雅干細(xì)胞技術(shù)有限公司

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LGK974，L974-002/010/050

LGK974，L974-002/010/050