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Home > Epigenetics Resch Products > EZH2 Methyltransferase Inhibitors > EPZ011989

EPZ011989

EPZ011989 is a cell permeable, metabolically stable and orally available EZH2 inhibitor, a compound with oral exposure and metabolic stability that is able to elicit robust methyl mark inhibition and antitumor activity. It binds potently and selectively to the mutant and wild-type EZH2 with Ki values < 3 nM, and highly selective over closely-related EZH1 (>15-fold selectivity) and 20 other histone methyltransferases (HMTs) (>3000-fold selectivity) tested. Demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with IC50s below 100 nM.

Catalog NO:	CT-EPZ989
Synonym:
CAS NO:	1598383-40-4
Mol. Formula:	C₃₅H₅₁N₅O₄ ∙HCl ∙ H₂O
MW:	660.3

** in vivo Quality material, * >99.5% by HPLC, a recrystallized pale yellow powder (pic attached). Clean and impeccable, with a spot-on quantitative microanalysis. Bulk stock, same day shipping.

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NO	Size	Price	In Stock	Quantity
1	10 mg	$80.00	YES
2	50 mg	$180.00	YES
3	100 mg	$280.00	YES
4	200 mg	$480.00	YES

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Solubility : Soluble in DMSO

Storage : Store at 0°C (short term), -20°C (long term), desiccated

Purity : >99.5% purity (HPLC at 214 and 254 nm)

Original QC Data : HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis Report

Please Pick Batch NO:

Current Lot, Certificate of Analysis
EPZ011989, Lot 01, Appearance (color).pdf

J. E. Campbell, et al, EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity, ACS Med Chem Lett. 2015 Mar 4;6 (5):491-495

*Clean and impeccable product, made for reproducible high quality research.

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