EPZ011989

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP15987CAS No. ：1598383-40-4Purity：98%

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CAS No.	1598383-40-4	Cat. No.	BCP15987
Name	EPZ011989
Synonyms	EPZ 011989;EPZ0-11989;
SMILES
Chemical Name
Formula	C35H51N5O4	M. Wt	605.81
Purity	98%	Storage	Store at 4-8°C
Description	In vitro: EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 dem