ORIC-944

Chemical Information
Rinzimetostat is an orally bioavailable allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. Upon oral administration, rinzimetostat targets and binds to the regulatory embryonic ectoderm development (EED) subunit of PRC2. This prevents the methyltransferase activity of PRC2, spefifically the methylation of histone 3 at lysine27 (H3K27). This depletes H3K27 trimethylation (H3K27me3) and modulates the expression of target genes. This may inhibit tumor cell proliferation. PRC2 is dysregulated in a variety of cancer cell types and is associated with poor prognosis. It is responsible for the methylation of H3K27 leading to transcriptional silencing. EED is essential for the histone methyltransferase activity of PRC2.
| CAS Number | 2369769-29-7 |
| PubChem CID | 155788096 |
| IUPAC Name | 8-[4-[(dimethylamino)methyl]-2-methylphenyl]-5-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]imidazo[1,2-c]pyrimidine-2-carbonitrile |
| Molecular Formula | C26H25FN6O |
| Molecular Weight | 456.5 |
| XLogP | 4.9 |
| Topological Polar Surface Area | 78.5 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 6 |
| Heavy Atom Count | 34 |
| Formal Charge | 0 |
| Complexity | 744 |
| Property | Value |
|---|---|
| Molecular Weight | 456.5 |
| XLogP3 | 4.9 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 6 |
| Exact Mass | 456.20738760 |
| Monoisotopic Mass | 456.20738760 |
| Topological Polar Surface Area | 78.5 Ų |
| Heavy Atom Count | 34 |
| Formal Charge | 0 |
| Complexity | 744 |
| 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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