1. Epigenetics
  2. Histone Methyltransferase
  3. EPZ011989

EPZ011989 

Cat. No.: HY-16986 Purity: 99.62%
Handling Instructions

EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.

For research use only. We do not sell to patients.

EPZ011989 Chemical Structure

EPZ011989 Chemical Structure

CAS No. : 1598383-40-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 280 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of EPZ011989:

Top Publications Citing Use of Products

Publications Citing Use of MCE EPZ011989

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase. IC50 value: < 3 nM ( Ki for wt EZH2, EZH2 Y646) Target: EZH2 inhibitor In vitro: 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. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.

Molecular Weight

605.81

Formula

C₃₅H₅₁N₅O₄

CAS No.

1598383-40-4

SMILES

O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#CCN3CCOCC3)=CC(N(CC)[[email protected]]4CC[[email protected]](N(CCOC)C)CC4)=C2C

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (165.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6507 mL 8.2534 mL 16.5068 mL
5 mM 0.3301 mL 1.6507 mL 3.3014 mL
10 mM 0.1651 mL 0.8253 mL 1.6507 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.62%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EPZ011989
Cat. No.:
HY-16986
Quantity: