EPZ011989 trifluoroacetate

Name: EPZ011989 trifluoroacetate
Brand: MedChemExpress
SKU: HY-16986A
Rating: 5.0 (2 reviews)

Cat. No.: HY-16986A: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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 K_i 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

CAS No. : 1598383-41-5

Size	Price	Stock	Quantity
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg		Get quote
50 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of EPZ011989 trifluoroacetate:

EPZ011989 In-stock
EPZ011989-d8 Get quote
EPZ011989 hydrochloride Get quote

2 Publications Citing Use of MCE EPZ011989 trifluoroacetate

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•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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 K_i 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 K_i 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	t_1/2 (h)	t_max (h)	C_max (ng/mL)	AUC_inf (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.

1598383-41-5

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.71%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (251 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[1]. Campbell JE, 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.3892 mL	6.9461 mL	13.8922 mL	34.7304 mL
	5 mM	0.2778 mL	1.3892 mL	2.7784 mL	6.9461 mL
	10 mM	0.1389 mL	0.6946 mL	1.3892 mL	3.4730 mL
	15 mM	0.0926 mL	0.4631 mL	0.9261 mL	2.3154 mL
	20 mM	0.0695 mL	0.3473 mL	0.6946 mL	1.7365 mL
	25 mM	0.0556 mL	0.2778 mL	0.5557 mL	1.3892 mL
	30 mM	0.0463 mL	0.2315 mL	0.4631 mL	1.1577 mL
	40 mM	0.0347 mL	0.1737 mL	0.3473 mL	0.8683 mL
	50 mM	0.0278 mL	0.1389 mL	0.2778 mL	0.6946 mL
	60 mM	0.0232 mL	0.1158 mL	0.2315 mL	0.5788 mL
	80 mM	0.0174 mL	0.0868 mL	0.1737 mL	0.4341 mL
	100 mM	0.0139 mL	0.0695 mL	0.1389 mL	0.3473 mL