Zamaporvint

Chemical Information
Zamaporvint is an orally available inhibitor of porcupine (PORCN), with potential antineoplastic activity. Upon oral administration, zamaporvint 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.
| CAS Number | 1900754-56-4 |
| PubChem CID | 121273514 |
| IUPAC Name | 2-[5-methyl-4-[2-(trifluoromethyl)-4-pyridinyl]imidazol-1-yl]-N-(5-pyrazin-2-yl-2-pyridinyl)acetamide |
| Molecular Formula | C21H16F3N7O |
| Molecular Weight | 439.4 |
| XLogP | 1.7 |
| Topological Polar Surface Area | 98.5 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 5 |
| Heavy Atom Count | 32 |
| Formal Charge | 0 |
| Complexity | 637 |
| Property | Value |
|---|---|
| Molecular Weight | 439.4 |
| XLogP3 | 1.7 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 5 |
| Exact Mass | 439.13684265 |
| Monoisotopic Mass | 439.13684265 |
| Topological Polar Surface Area | 98.5 Ų |
| Heavy Atom Count | 32 |
| Formal Charge | 0 |
| Complexity | 637 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 1 |
| Compound Is Canonicalized | Yes |
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