产品信息
抗原名称
Porcn
商品描述
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.
分子量
396.44
纯度
>98%
可溶性
DMSO : 73 mg/mL (184.1 mM)
外观
White to Off-White Solid
In vitro(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.
In vivo(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.
背景
别名
LGK 974；WNT974；LGK-974；NVP-LGK974
分子式
C23H20N6O
CAS号
1243244-14-5
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
本文来自投稿，不代表本人立场，如若转载，请注明出处：http://www.iamyjet.com/article/21558.html