EPZ-011989 trifluoroacetate ( EPZ011989 trifluoroacetate )

Catalog No. M12290 CAS No. 1598383-41-5

COA

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HNMR

HPLC

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Product Name

EPZ-011989 trifluoroacetate
Note

Research use only, not for human use.
Brief Description

A potent, selective, orally bioavailable inhibitor of EZH2 with Ki of < 3 nM.
Description

A potent, selective, orally bioavailable inhibitor of EZH2 with Ki of < 3 nM; equipotently inhibits mutant and wild-type EZH2, displays >15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTs; demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.Blood Cancer Preclinical
Synonyms

EPZ011989 trifluoroacetate
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

Cancer
Indication

Blood cancer

CAS Number

1598383-41-5
Formula Weight

719.83
Molecular Formula

C37H52F3N5O6
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 34 mg/mL
SMILES

COCCN([C@@H]1CC[C@@H](N(C2=CC(C#CCN3CCOCC3)=CC(C(NCC4=C(C)C=C(C)NC4=O)=O)=C2C)CC)CC1)C.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
Chemical Name

Benzamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl[trans-4-[(2-methoxyethyl)methylamino]cyclohexyl]amino]-2-methyl-5-[3-(4-morpholinyl)-1-propyn-1-yl]-, 2,2,2-trifluoroacetate (1:x)

1. Campbell JE, et al. ACS Med Chem Lett. 2015 Mar 4;6(5):491-5.
2. Gardner EE, et al. Cancer Cell. 2017 Feb 13;31(2):286-299.

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