FX-909

Chemical Information
PPAR Gamma Inhibitor FX-909 is an orally available inverse agonist and inhibitor of the transcription factor (TF) peroxisome proliferator-activated receptor gamma (PPAR gamma; PPARG), with potential antineoplastic activity. Upon oral administration, PPARG inhibitor FX-909 selectively targets and covalently binds to a region of PPARG that is sequestered from the mutation site. The binding promotes a repressive conformation of PPARG and inhibits the activity of PPARG. This inhibits both basal- and ligand-activated transcription by PPARG and prevents PPARG-mediated transcription of target genes, such as FABP4/Fabp4, AGT/Agt, IVT/Ivd and ARG1/Arg1. This may inhibit proliferation in PPARG-overactivated tumor cells. PPARG, a nuclear receptor, is genetically altered, including amplification, missense mutations, and fusions, in certain tumor cells commonly associated with the luminal lineage subtype.
| CAS Number | 2924573-90-8 |
| PubChem CID | 167993670 |
| IUPAC Name | 3-(5,7-difluoro-4-oxo-1H-quinolin-2-yl)-4-methylsulfonylbenzonitrile |
| Molecular Formula | C17H10F2N2O3S |
| Molecular Weight | 360.3 |
| XLogP | 2.4 |
| Topological Polar Surface Area | 95.4 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 2 |
| Heavy Atom Count | 25 |
| Formal Charge | 0 |
| Complexity | 737 |
| Property | Value |
|---|---|
| Molecular Weight | 360.3 |
| XLogP3 | 2.4 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 2 |
| Exact Mass | 360.03801968 |
| Monoisotopic Mass | 360.03801968 |
| Topological Polar Surface Area | 95.4 Ų |
| Heavy Atom Count | 25 |
| Formal Charge | 0 |
| Complexity | 737 |
| 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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