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抑制剂描述:

产品名称:LGK-974

产品别名:见爱必信官网

英文别名:LGK-974

靶点:PORCN

CAS:1243244-14-5

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 <1 nM in the Wnt signaling reporter assay and Porcupine binding assay.

溶解性:DMSO Solubility: 79 mg/mL warmed (199.27 mM)

体外研究:

LGK974 effectively displaces -GNF-1331 with IC50 of 1 nM in the PORCN radioligand binding assay, and shows no major cytotoxicity in cells up to 20 μM. LGK974 shows comparable inhibitory activities against all tested Wnts with IC50 ranging from 0.05 to 2.4 nM, which is consistent with the genetic loss of PORCN phenotype. LGK974 specifically inhibits the growth of three RNF43-mutant cell lines, HPAF-II, PaTu 8988S, and Capan-2.

体内研究:In a murine MMTV-Wnt1 tumor model and a human head and neck squamous cell carcinoma model (HN30), LGK974 (3 mg/kg) inhibits Wnt signaling in vivo and induces tumor regression without significant body weight loss in the mice. LGK974 (5 mg/kg, p.o., BID) also inhibits tumor growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2) in vivo.

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