EPZ-6438 (TAZEMETOSTAT)

Background Information:

EPZ6438 (Tazemetostat, E7438) is an orally bioactive, potent,
selective and S-adenosyl methionine (SAM) competitive inhibitor of
Histone Methyltransferase (HMT) EZH2 with a Ki = 2.5 nM for wild type
EZH2. The compound potently inhibits all known mutants of EZH2 that have
been identified in non-Hodgkin lymphoma (NHL) patient samples. It has
greater than 4500-fold selectivity against other 14 HMTs tested and
35-fold selectivity against the closely related enzyme EZH1.

Reference:

1. S. K. Knutson, et al., Durable tumor regression in genetically
altered malignant rhabdoid tumors by inhibition of methyltransferase
EZH2. Proc Natl Acad Sci U S A. 2013 May 7, 110(19), 7922-7.

APIM050328: EPZ-6438 (TAZEMETOSTAT)

CAS No.: 1403254-99-8.
Molecular Formula: C₃₄H₄₄N₄O₄ ? 0.4HCl.
Molecular Weight: 587.3.
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.