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Product name : LGK-974
Item : CR1864
Price : 100mg, $945; 200mg, $1485
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Additional Information :  We offer significant discount for bulky quantity order,Please ask price and availability of other quantities
CAS : 1243244-14-5
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Details:
 Chemical Information
M.Wt 396.44 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C23H20N6O
CAS No 1243244-14-5
Solubility

DMSO 79 mg/ml; Water <1 mg/ml



Biological Activity of LGK974

 

LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.
IC50 value: 0.4 nM [1]
Target: Porcupine
in vitro: LGK974 effectively displaces [3H]-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 [1]. LGK974 specifically inhibits the growth of three RNF43-mutant cell lines, HPAF-II, PaTu 8988S, and Capan-2 [2].
in vivo: 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 [1]. LGK974 (5 mg/kg, p.o., BID) also inhibits tumor growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2) in vivo [2].

 

[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]. Jiang X, et al. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma. Proc Natl Acad Sci U S A. 2013 Jul 30;110(31):12649-54.


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