LGK974
LGK974
CAS: 1243244-14-5
Molecular Formula: C23H20N6O
LGK974 - Names and Identifiers
| Name | LGK974 |
| Synonyms | LGK974 LGK-974 CS-1102 LGK-974 MK-0991, L-743872 LGK974(NVP-LGK974) 2',3-Dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-[2,4'-bipyridine]-5-acetamide 2-(2',3-Dimethyl-2,4'-bipyridin-5-yl)-N-[5-(2-pyrazinyl)-2-pyridi nyl]acetamide 2-(2',3-diMethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetaMide 2-[5-Methyl-6-(2-methyl-4-pyridyl)-3-pyridyl]-N-(5-pyrazin-2-yl-2-pyridyl)acetamide |
| CAS | 1243244-14-5 |
LGK974 - Physico-chemical Properties
| Molecular Formula | C23H20N6O |
| Molar Mass | 396.44 |
| Density | 1.268±0.06 g/cm3(Predicted) |
| Melting Point | 176 - 180°C |
| Boling Point | 650.9±55.0 °C(Predicted) |
| Solubility | soluble in DMSO |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 12.24±0.70(Predicted) |
| Storage Condition | Refrigerator |
| Use | LGK974 (WNT974) is a potent, orally active, specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM. |
| In vitro study | LGK-974 in the PORCN radioligand binding assay, the [LGK974 can be effectively substituted to specifically inhibit the growth of three RNF43 mutant cell lines HPAF-II, PaTu 8988S, and Capan-2. |
| In vivo study | LGK-974 (3 mg/kg) inhibits Wnt signaling pathway in mouse MMTV-WNT1 tumor model and human head and neck squamous cell carcinoma model (hn30), tumor regression was induced and there was no significant decrease in body weight of the mice. LGK-974 (5 mg/kg, p.o., BID) also inhibited the growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2). |
LGK974 - Reference
| Reference Show more | 1: Liu J, Pan S, Hsieh MH, Ng N, Sun F, Wang T, Kasibhatla S, Schuller AG, Li AG, Cheng D, Li J, Tompkins C, Pferdekamper A, Steffy A, Cheng J, Kowal C, Phung V, Guo G, Wang Y, Graham MP, Flynn S, Brenner JC, Li C, Villarroel MC, Schultz PG, Wu X, McNamara P, Sellers WR, Petruzzelli L, Boral AL, Seidel HM, McLaughlin ME, Che J, Carey TE, Vanasse G, Harris JL. 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. doi: 10.1073/pnas.1314239110. Epub 2013 Nov 25. PubMed PMID: 24277854; PubMed Central PMCID: PMC3864356. 2: Jiang X, Hao HX, Growney JD, Woolfenden S, Bottiglio C, Ng N, Lu B, Hsieh MH, Bagdasarian L, Meyer R, Smith TR, Avello M, Charlat O, Xie Y, Porter JA, Pan S, Liu J, McLaughlin ME, Cong F. 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. doi: 10.1073/pnas.1307218110. Epub 2013 Jul 11. PubMed PMID: 23847203; PubMed Central PMCID: PMC3732970. |
LGK974 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.522 ml | 12.612 ml | 25.224 ml |
| 5 mM | 0.504 ml | 2.522 ml | 5.045 ml |
| 10 mM | 0.252 ml | 1.261 ml | 2.522 ml |
| 5 mM | 0.05 ml | 0.252 ml | 0.504 ml |
Last Update：2024-01-02 23:10:35
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