EPZ011989

Catalog No.S7805

EPZ011989 Chemical Structure

Molecular Weight(MW): 642.27

EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM.

Size Price Stock Quantity  
USD 97 In stock
USD 297 In stock
USD 677 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM.
Targets
EZH2 [1]
(Cell-free assay)
EZH1 [1]
(Cell-free assay)
<3 nM(Ki) 103 nM
In vitro

EPZ011989 equipotently inhibits mutant and wild-type EZH2 with an inhibition constant (Ki) of <3 nM. 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. As evidenced by the human and rat liver microsomal turnover, EPZ011989 also exhibits metabolic stability. EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM[1]. EPZ011989 inhibits H3K27me3 in wild-type EZH2 AML cell lines (Kasumi-1, MOLM-13, and MV4-11) at a concentration of 0.625 μM after only four days of treatment. At these concentrations and this time point, no change in viability among these three cell lines is observed and only minimal proliferation inhibition in MV4-11 and MOLM-13 cells[2].

In vivo EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. EPZ011989 is able to elicit robust methyl mark inhibition and antitumor activity[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: WSU-DLCL2 cells
  • Concentrations: 0-10 μM
  • Incubation Time: 0-11 days
  • Method:

    For assessment of cell proliferation and viability, exponentially growing cells are plated, in triplicate, in 96-well plates. Cells are incubated with increasing concentrations of EPZ011989. Viable cell number is determined every 3-4 days for up to 11 days using the Guava Viacount assay.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: SCID mice
  • Formulation: 0.5% methyl cellulose and 0.1% Tween-80
  • Dosages: 250 and 500 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 100 mg/mL (155.69 mM)
DMSO Insoluble
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 642.27
Formula

C35H51N5O4·HCl

CAS No. 1598383-40-4(free base)
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Related Antibodies

Histone Methyltransferase Signaling Pathway Map

Tags: buy EPZ011989 | EPZ011989 supplier | purchase EPZ011989 | EPZ011989 cost | EPZ011989 manufacturer | order EPZ011989 | EPZ011989 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID