EPZ011989 | B1221

EPZ011989 is a potent EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutated EZH2. It displays 15-fold selectivity for EZH2 over EZH1 and is without effect against an array of other lysine methyltransferases. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.

EPZ011989 is a potent EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutated EZH2. It displays 15-fold selectivity for EZH2 over EZH1 and is without effect against an array of other lysine methyltransferases. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.

B1221 | EPZ011989 DataSheet

Alternate Name/Synonyms: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl((1r,4r)-4-((2-methoxyethyl)(methyl)amino)cyclohexyl)amino)-2-methyl-5-(3-morpholinoprop-1-yn-1-yl)benzamide

Appearance: Off-white solid

Formulation: N/A

CAS Number: 1598383-40-4

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₃₅H₅₁N₅O₄

Molecular Weight: 605.82

Cell-Permeable?: Yes

Purity: 95% by HPLC

Solubilities: DMSO(>10 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent EZH2 inhibitor

MDL Number: N/A

PubChem CID: 73670548

SMILES: CCN(C1CCC(CC1)N(C)CCOC)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C#CCN4CCOCC4

InChi: InChI=1S/C35H51N5O4/c1-7-40(30-12-10-29(11-13-30)38(5)15-18-43-6)33-23-28(9-8-14-39-16-19-44-20-17-39)22-31(27(33)4)34(41)36-24-32-25(2)21-26(3)37-35(32)42/h21-23,29-30H,7,10-20,24H2,1-6H3,(H,36,41)(H,37,42)

InChi Key: XQFINGFCBFHOPE-UHFFFAOYSA-N