1. Epigenetics
  2. Histone Methyltransferase
  3. EPZ011989

EPZ011989 

Cat. No.: HY-16986 Purity: 99.00%
COA Handling Instructions

EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers.

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

EPZ011989 Chemical Structure

EPZ011989 Chemical Structure

CAS No. : 1598383-40-4

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Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
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5 mg USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 99 In-stock
Estimated Time of Arrival: December 31
50 mg USD 308 In-stock
Estimated Time of Arrival: December 31
100 mg USD 495 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of EPZ011989:

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Description

EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers[1].

IC50 & Target

Ki: <3 nM (EZH2); IC50: 94 nM (H3K27 methylation inhibition)[1].

In Vitro

EPZ011989 inhibits mutant and wild-type EZH2 with an Ki value of <3 nM[1].
EPZ011989 reduces cellular H3K27 methylation with an IC50 value of 94 nM[1].
EPZ011989 (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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

EPZ011989 (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice[1]
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.
Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time.
Animal Model: Rat[1]
Dosage: 30, 100, and 300 mg/kg
Administration: Oral, single
Result:
dose (mg/kg) route t1/2 (h) tmax (h) Cmax (ng/mL) AUCinf (h*ng/mL) time above LCC (h)
30 p.o. 4.7 2 240 970 4
100 p.o. 3.9 2.7 1600 5600 8
300 p.o. 3.7 2.7 2900 10000 10
Molecular Weight

605.81

Formula

C35H51N5O4

CAS No.
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 available by MCE.
Purity & Documentation

Purity: 99.00%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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