ARV-393

Chemical Information
Zaloblideg is an orally bioavailable, targeted degrader composed of an E3 ubiquitin ligase-binding moiety that is conjugated, via a linker, to a B-cell lymphoma 6 protein (BCL6; BCL-6)-binding moiety using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. Upon oral administration of zaloblideg, the BCL6-binding moiety specifically targets and binds to BCL6 on tumor cells while the E3 ubiquitin ligase-binding moiety targets and binds to E3 ubiquitin ligase, thereby creating a ternary complex. This induces E3 ligase ubiquitination and proteasome-mediated degradation of BCL6. This prevents BCL6-mediated signaling and activation of downstream survival pathways. This leads to an inhibition of the growth of tumor cells that overexpress BCL6. BCL6, a transcriptional repressor overexpressed in certain tumor cells, serves an important role in cell signaling and tumor cell proliferation.
| CAS Number | 2851885-95-3 |
| PubChem CID | 166077922 |
| IUPAC Name | 2-[6-[[5-chloro-2-[4-[3-[4-[2-(2,6-dioxopiperidin-3-yl)-4-fluoro-1-oxo-3H-isoindol-5-yl]piperidin-1-yl]cyclobutyl]oxypiperidin-1-yl]pyrimidin-4-yl]amino]-2-oxo-1-propan-2-ylquinolin-3-yl]oxy-N-methylacetamide |
| Molecular Formula | C46H53ClFN9O7 |
| Molecular Weight | 898.4 |
| XLogP | 4.7 |
| Topological Polar Surface Area | 179 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 13 |
| Rotatable Bond Count | 12 |
| Heavy Atom Count | 64 |
| Formal Charge | 0 |
| Complexity | 1770 |
| Property | Value |
|---|---|
| Molecular Weight | 898.4 |
| XLogP3 | 4.7 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 13 |
| Rotatable Bond Count | 12 |
| Exact Mass | 897.3740509 |
| Monoisotopic Mass | 897.3740509 |
| Topological Polar Surface Area | 179 Ų |
| Heavy Atom Count | 64 |
| Formal Charge | 0 |
| Complexity | 1770 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 1 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 1 |
| Compound Is Canonicalized | Yes |
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