Network Version
LGK974 Data Sheet
| Product Name: | LGK974 |
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|---|---|---|
| CAS No.: | 1243244-14-5 | |
| Cat. No.: | HY-17545 | |
| MWt: | 396.44 | |
| Formula: | C23H20N6O | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 32 mg/mL (80.72 mM) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM[1]. IC50 & Target: Porcupine[1] In Vitro: 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[1]. In Vivo: 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[1]. | ||
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