2-(2',3-Dimethyl-[2,4'-Bipyridin]-5-Yl)-N-(5-(Pyrazin-2-Yl)Pyridin-2-Yl)Acetamide 2-(2',3-二甲基-[2,4'-联吡啶]-5-基)-N-(5-(吡嗪-2-基)吡啶-2-基)乙酰胺
CAS 1243244-14-5 MFCD343244145
化学结构图
SMILES: Cc1cc(-c2ncc(CC(=O)Nc3ccc(-c4cnccn4)cn3)cc2C)ccn1
化学属性
| Density | |
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| Boiling Point | |
| Melting Point | |
| Mol. Weight | 396 |
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
| Mol. Formula | C23H20N6O |
别名和识别编码
| Synonym | 2-(2',3-Dimethyl-(2,4'-bipyridin)-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide LGK-974 LGK974 LGK974; LGK-974; LGK 974; WNT974; WNT 974; WNT-974 WNT-974 WNT974 |
|---|---|
| EC Number | |
| Beilstein Registry Number | |
| Chemical Name Translation | 2-(2',3-二甲基-[2,4'-联吡啶]-5-基)-N-(5-(吡嗪-2-基)吡啶-2-基)乙酰胺 |
| LabNetwork Molecule ID | LN00218237 |
| Chemical Name | 2-(2',3-Dimethyl-[2,4'-Bipyridin]-5-Yl)-N-(5-(Pyrazin-2-Yl)Pyridin-2-Yl)Acetamide |
| PubChem Substance ID | 46926973 |
| InChI | InChI=1S/C23H20N6O/c1-15-9-17(12-28-23(15)18-5-6-25-16(2)10-18)11-22(30)29-21-4-3-19(13-27-21)20-14-24-7-8-26-20/h3-10,12-14H,11H2,1-2H3,(H,27,29,30) |
| Formula | C23H20N6O |
| IUPAC Name | 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide |
| InChIKey | XXYGTCZJJLTAGH-UHFFFAOYSA-N |
| Canonical SMILES | O=C(NC1=NC=C(C2=NC=CN=C2)C=C1)CC3=CN=C(C4=CC(C)=NC=C4)C(C)=C3 |
| MDL Number | |
| CAS Number | 1243244-14-5 |
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产品应用
- LGK974, also known as WNT974, is a selective and orally bioavailable porcupine (PORCN) inhibitor under development for the treatment of cancers that are driven by the Wnt pathway in a Wnt ligand-dependent manner. WNT974 binds to and inhibits PORCN in the endoplasmic reticulum (ER), which blocks post-translational acylation of Wnt ligands and inhibits their secretion. This prevents the activation of Wnt ligands, interferes with Wnt-mediated signaling, and inhibits cell growth in Wnt-driven tumors. Porcupine, a membrane-bound O-acyltransferase (MBOAT), is required for the palmitoylation of Wnt ligands, and plays a key role in Wnt ligand secretion and activity. Wnt signaling is dysregulated in a variety of cancers.
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