MRT-2359

Chemical Information
GSPT1 MGD MRT-2359 is an orally bioavailable selective molecular glue degrader (MGD) of the translational termination factor GSPT1, with potential antineoplastic activity. Upon oral administration, MRT-2359 targets and binds to GSPT1, thereby promoting complex formation between the E3 ubiquitin ligase component cereblon (CRBN) and GSPT1, and inducing GSPT1 degradation in a CRBN- and degron-dependent manner. This downregulates L-MYC and N-MYC, thereby disrupting MYC-driven protein translation and reducing MYC-oncogenic signaling. This inhibits proliferation in MYC-driven tumors. The translation termination factor GSPT1, a G-loop degron-containing protein, plays a key role in protein translation in MYC-driven cancers.
| CAS Number | 2803881-11-8 |
| PubChem CID | 164584214 |
| IUPAC Name | [2-(2,6-dioxopiperidin-3-yl)-3-oxo-1H-isoindol-5-yl]methyl N-[2-fluoro-5-(trifluoromethoxy)phenyl]carbamate |
| Molecular Formula | C22H17F4N3O6 |
| Molecular Weight | 495.4 |
| XLogP | 2.5 |
| Topological Polar Surface Area | 114 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 6 |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 856 |
| Property | Value |
|---|---|
| Molecular Weight | 495.4 |
| XLogP3 | 2.5 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 6 |
| Exact Mass | 495.10534792 |
| Monoisotopic Mass | 495.10534792 |
| Topological Polar Surface Area | 114 Ų |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 856 |
| 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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