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S80215

LGK974

源叶(MedMol) 98%
  • 英文名:
  • LGK974
  • 别名:
  • CAS号:
  • 1243244-14-5
  • 分子式:
  • C23H20N6O
  • 分子量:
  • 396.4445
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S80215-5mg 98% ¥880.00元 6 - - - EA 加入购物车
源叶(MedMol) S80215-10mg 98% ¥1496.00元 2 - - - EA 加入购物车
源叶(MedMol) S80215-50mg 98% ¥4400.00元 1 - - - EA 加入购物车
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参考文献

质检证书(COA)

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  • 提示:详情请下载说明书。
  • 产品描述: LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM
  • 靶点: Porcupine
  • 体外研究:
    LGK974 effectively displaces [3H]-GNF-1331 with an IC50 of 1 nM in the PORCN radioligand binding assay. LGK974 potently reduces Wnt-dependent AXIN2 mRNA levels in HN30 cells with an IC50 of 0.3 nM.
  • 体内研究:
    LGK974, a drug that targets Porcupine, a Wnt-specific acyltransferase. LGK974 potently inhibits Wnt signaling, has strong efficacy in rodent tumor models, and is well-tolerated. Toxicology studies are performed on nontumor bearing rats at 3 and 20 mg/kg. At the efficacious dose of 3 mg/kg per day for 14 d, LGK974 is well-tolerated without abnormal histopathological findings in Wnt-dependent tissues, including the intestine, stomach, and skin. When rats are administrated a very high dose of 20 mg/kg per day for 14 d, loss of intestinal epithelium is observed, consistent with the concept that Wnt is required for intestinal tissue homeostasis.
  • 参考文献:
    1. Liu J, et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proc Natl Acad Sci U S A. 2013 Dec 10;110(50):20224-9. 2. Tammela T, et al. A Wnt-producing niche drives proliferative potential and progression in lung adenocarcinoma. Nature. 2017 May 18;545(7654):355-359.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.522 ml 12.612 ml 25.224 ml
    5 mM 0.504 ml 2.522 ml 5.045 ml
    10 mM 0.252 ml 1.261 ml 2.522 ml
    50 mM 0.05 ml 0.252 ml 0.504 ml
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