Zeprumetostat, also known as SHR2554, is a small-molecule inhibitor of enhancer of zeste homolog 2 (EZH2) and belongs to the class of compounds investigated for antineoplastic applications. Its chemical identity is documented under CAS No. 2098545-98-1, with the molecular formula C₃₂H₄₄N₄O₄ and molecular weight approximately 548.73 g/mol.
Zeprumetostat is associated with inhibition of the catalytic activity of EZH2, an enzyme involved in histone methylation and epigenetic regulation. EZH2 is a catalytic component of the Polycomb Repressive Complex 2 (PRC2), and abnormal EZH2 activity has been investigated in several hematological and solid tumor settings. Zeprumetostat has therefore been studied as a targeted small-molecule compound for oncology research and pharmaceutical development.
The International Nonproprietary Name documentation identifies zeprumetostat as an EZH2 inhibitor and antineoplastic compound. The WHO documentation also provides the chemical structure, molecular formula and CAS-associated identifier 2098545-98-1.
Zeprumetostat has the systematic chemical name:
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-5-ethyl-6-[ethyl(oxan-4-yl)amino]-2-(piperidin-1-ylmethyl)-1-benzofuran-4-carboxamide
Its molecular formula is C₃₂H₄₄N₄O₄, while its molecular weight is approximately 548.72–548.73 g/mol. The compound is also identified by the development code SHR2554 and has been referenced as EZH2-IN-15 in chemical and research literature.
The compound contains a benzofuran carboxamide structural framework together with substituted pyridinone, piperidine and oxane-related structural components. Its physicochemical profile includes a calculated XLogP value around 3.59 in the IUPHAR database.
Zeprumetostat is of interest to pharmaceutical research organizations working on EZH2-targeted therapies, oncology drug discovery, formulation development and analytical research. Research data indicate that SHR2554 inhibits both wild-type and selected mutant forms of EZH2 methyltransferase activity.
Available research data report activity against EZH2 and demonstrate reduction of intracellular H3K27me3 levels in relevant experimental models. These findings have supported investigation of zeprumetostat in oncology research, including studies involving lymphoid neoplasms.
For pharmaceutical and research organizations, appropriate characterization of Zeprumetostat includes identity confirmation, chromatographic purity assessment, impurity profiling, residual solvent evaluation and other analytical controls appropriate to the intended use. Because publicly available specifications can differ between research-grade material and pharmaceutical-grade API, the final release specification should always be established against the applicable product dossier, validated analytical method and batch-specific Certificate of Analysis.
Zeprumetostat is reported as a solid powder in available research documentation. A commercial research-material COA reports HPLC/LCMS purity greater than 98%, with HPLC and NMR analytical results described as consistent with the compound identity. This value should be treated as a documented research-material analytical result, rather than a universal pharmaceutical specification.
Available chemical supplier information also reports Zeprumetostat as slightly soluble in acetonitrile at approximately 0.1–1 mg/mL, while another technical data source reports a 10 mM solution in DMSO. Solubility can vary according to solvent, concentration, temperature and material characteristics, so formulation or analytical development should use experimentally verified data.
For pharmaceutical development, analytical characterization may include HPLC or UPLC assay, LC-MS identification, NMR characterization, related substances, residual solvents, water content, elemental impurities and other quality attributes defined by the applicable specification. Batch-specific analytical documentation should be consulted before commercial pharmaceutical use.
Swapnroop Drugs and Pharmaceuticals positions its business around pharmaceutical raw materials, APIs, excipients and global pharmaceutical supply, with a stated WHO-GMP-certified manufacturing and export focus. The company's website states that it serves pharmaceutical manufacturers, formulation companies, research laboratories and other organizations across international markets.
For Zeprumetostat-related requirements, pharmaceutical companies, research organizations and formulation-development teams can evaluate the required grade, quantity, analytical specification and documentation according to their intended application. Relevant quality documentation may include Certificate of Analysis, Safety Data Sheet, analytical reports and other regulatory documentation where applicable.
Zeprumetostat is primarily associated with EZH2-targeted pharmaceutical research and oncology drug development. Research involving this compound has examined EZH2 methyltransferase inhibition, H3K27me3 modulation and anti-proliferative effects in experimental cancer models.
Potential research and development areas include:
Zeprumetostat should not be described as universally pharmacopeial-grade or marketed for a particular therapeutic use unless the applicable regulatory and product documentation supports that statement.
Consistent quality control is important for pharmaceutical development involving novel or recently developed APIs. Buyers evaluating Zeprumetostat should consider identity, assay, related substances, residual solvents, elemental impurities, water content, physical characteristics and stability requirements.
The appropriate specification should be agreed according to the intended application and regulatory market. Documentation requirements may differ between research, development, clinical and commercial pharmaceutical applications.
For bulk Zeprumetostat API requirements, organizations can provide their desired specification, quantity, grade and documentation requirements for technical evaluation and sourcing.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 98.0% |