LGK-974
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 PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18940261
| Cas No. |
1243244-14-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C23H20N6O |
| Formula Wt. |
396.44 |
| IUPAC Name |
2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide |
| Synonym |
LGK974 |
| Appearance |
White to off white powder |
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.
