1. Epigenetics
  2. Histone Methyltransferase
  3. EPZ011989 trifluoroacetate

EPZ011989 trifluoroacetate 

Cat. No.: HY-16986A
COA Handling Instructions

EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers. EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

EPZ011989 trifluoroacetate Chemical Structure

EPZ011989 trifluoroacetate Chemical Structure

CAS No. : 1598383-41-5

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of EPZ011989 trifluoroacetate:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers[1]. EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

EZH2

 

In Vitro

EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an Ki value of <3 nM[1].
EPZ-011989 trifluoroacetate reduces cellular H3K27 methylation with an IC50 value of 94 nM[1].
EPZ-011989 trifluoroacetate (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells[1].

MedChemExpress (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

EPZ-011989 trifluoroacetate (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity[1].

MedChemExpress (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

719.83

Formula

C37H52F3N5O6

CAS No.
Appearance

Solid

Color

Light yellow to yellow

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.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (138.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3892 mL 6.9461 mL 13.8922 mL
5 mM 0.2778 mL 1.3892 mL 2.7784 mL
10 mM 0.1389 mL 0.6946 mL 1.3892 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 (3.47 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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EPZ011989 trifluoroacetate Related Classifications

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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EPZ011989 trifluoroacetate
Cat. No.:
HY-16986A
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