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Cat. Number
L2540
Chemical Name
L2540 LGK-974 1243244-14-5
CAS Number
1243244-14-5
Mol. Formula
C23H20N6O
Mol. Weight
396.44
Qty 1
1mg
Qty 2
5mg
Appearance
White to off white powder
Application Notes
≥98%
Synonym
LGK974
Solubility
DMSO 79 mg/mL warmed (199.27 mM) Water Insoluble Ethanol Insoluble
Storage condition
-20°C
References

LGK-974 inhibits PORCN, suppressing Wnt signaling. This compound exhibits anticancer chemotherapeutic activity and is currently in clinical trials. LGK-974 inhibits proliferation and induces differentiation of pancreatic adenocarcinoma xenografts; it also shows efficacy in suppressing tumor growth in animal models of breast cancer and squamous cell carcinoma.

References

Liu J, Pan S, Hsieh MH, 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. PMID: 24277854.

Jiang X, Hao HX, Growney JD, 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. PMID: 23847203.

Jang J, Song J, Lee H, et al. LGK974 suppresses lipopolysaccharide-induced endotoxemia in mice by modulating the crosstalk between the Wnt/beta-catenin and NF-kB pathways. Exp Mol Med. 2021 Mar;53(3):407-421. PMID: 33692475.


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