EPZ-6438 is a potent, selective and orally bioavailable inhibitor of methyltransferase EZH2 with a Ki value of 2.5 nM. EPZ-6438 also shows a 35-fold selectivity versus EZH1 (IC50 392 nM) and >4,500-fold selectivity relative to 14 other histone methyltransferases (HMTs). [1] Oral dosing of EPZ-6438 leads to potent antitumor activity in a SMARCB1-deleted malignant rhabdoid tumor (MRT) xenograft model. [1]
EPZ-6438 is being studied in Phase III clinical trials in patients with diffuse large B-cell lymphoma [2] and relapsed/refractory synovial sarcoma [3].
Technical information:
| Chemical Formula: | C34H44N4O4 | |
| CAS #: | 1403254-99-8 | |
| Molecular Weight: | 572.74 | |
| Purity: | > 98% | |
| Appearance: | Off-white | |
| Chemical Name: | N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide | |
| Solubility: | Up to 10 nM in DMSO | |
| Synonyms: | EPZ-6438, EPZ6438, Tazemetostat |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci U S A. 2013; 110(19):7922-7 Pubmed ID: 23620515 |
| 2. | Open-Label, Multicenter, Phase 1/2 Study of Tazemetostat (EZH2 Histone Methyl Transferase [HMT] Inhibitor) as a Single Agent in Subjects With Adv. Solid Tumors or With B-cell Lymphomas and Tazemetostat in Combination With Prednisolone in Subjects With DLBCL. clinicaltrials.gov/NCT01897571 |
| 3. | A Phase II, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adult Subjects With INI1-Negative Tumors or Relapsed/Refractory Synovial Sarcoma. clinicaltrials.gov/NCT02601950 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.