EPZ-011989( EPZ011989 )

Catalog No. M12289 CAS No. 1598383-40-4

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Datasheet

HNMR

HPLC

MSDS

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Product Name

EPZ-011989
Note

Research use only, not for human use.
Brief Description

EPZ-011989 (EPZ011989) is a potent, selective, orally bioavailable inhibitor of EZH2 with Ki of < 3 nM.
Description

EPZ-011989 (EPZ011989) is 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.
In Vitro

Cell Proliferation Assay Cell Line:WSU-DLCL2 cells Concentration:0-10 μM Incubation Time:11 days Result:Demonstrated an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM.
In Vivo

Animal Model:SCID mice Dosage:125, 250, 500, and 1000 mg/kg Administration:Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days Result:Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h.Observed complete ablation of the methyl mark by the end of day 7.
Synonyms

EPZ011989
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

EZH2
Research Area

Cancer
Indication

Blood cancer

CAS Number

1598383-40-4
Formula Weight

605.8105
Molecular Formula

C35H51N5O4
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 33 mg/mL
SMILES

O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#CCN3CCOCC3)=CC(N(CC)[C@H]4CC[C@H](N(CCOC)C)CC4)=C2C
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]-

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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