EPZ5676

EPZ5676 is a potent inhibitor of DOT1L histone methyltransferase that, according to X-ray crystallographic analysis, occupies the S-adenosyl methionine (SAM) binding pocket of DOT1L and induces conformational changes in DOT1L resulting in the opening of a hydrophobic pocket beyond the amino acid portion of SAM. EPZ5676 has been investigated for the treatment of MLL-rearranged leukemia in multiple studies where results have shown that EPZ5676 inhibits H3K79 methylation and the expression of MLL-fusion target gene and potently kills acute leukemia cell lines bearing MLL translocation.

≥ 28.15 mg/mL in DMSO; insoluble in H2O; ≥ 50.3 mg/mL in EtOH with ultrasonic. For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Long-term storage in solution is not recommended. Not stable in diluted solutions.

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.