Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal 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
Purity: ≥98%
Formula Markup: C34H44N4O4
Formula Weight: 572.7
CAS Number: 1403254-99-8
Notes: EPZ6438 is an orally bioavailable, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 2.5 nM), the enzymatic subunit of polycomb repressive complex 2.{28475} It displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other histone methyltransferases.{28475} EPZ6438 blocks histone H3 lysine 27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM).{28476} EPZ6438 has been shown to induce apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and to promote their regression in xenograft-bearing mice.{28475}
Deutsch
English
