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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.
| Cas No. | 1243244-14-5 |
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| Purity | ≥98% |
| Formula | C23H20N6O |
| Formula Wt. | 396.44 |
| Chemical Name | 2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide |
| IUPAC Name | 2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide |
| Synonym | LGK974 |
| Solubility | DMSO 79 mg/mL warmed (199.27 mM) Water Insoluble Ethanol Insoluble |
| Appearance | White to off white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet | |
| Brochures |
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.