Cat. No.: HY-139626

EPZ-719

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

EPZ-719 is a selective, orally effective SETD2 inhibitor with an IC₅₀ value of 0.005 μM. EPZ-719 has anticancer activity.

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

Purity: 99.00%
CAS No.: 2697176-16-0
Formula: C₂₂H₃₁FN₄O₃S
Molecular Weight:450.57

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

EPZ-719 Chemical Structure

CAS No.: 2697176-16-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

EPZ-719 is a selective, orally effective SETD2 inhibitor with an IC₅₀ value of 0.005 μM. EPZ-719 has anticancer activity^[1].

IC₅₀ & Target

SETD2/KMT3A

All Histone Methyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
KMS-11	IC₅₀	0.211 μM Compound: 32; EPZ-719	Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by LTP assay Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by LTP assay	[PMID: 34671445]

In Vitro

EPZ-719 (14 days) can inhibit cell proliferation in KMS34 and KMS11 cells with IC₅₀ values of 0.025 μM and 0.211 μM, respectively^[1].

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

In Vivo

Pharmacokinetic parameters in rats^[1]

T_1/2(h)	CL (mL/min/kg)	V_ss(L/kg)
3.13	53.3	8.13

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

Chemical Information

CAS No. 2697176-16-0
Appearance Solid
Molecular Weight 450.57
Formula C₂₂H₃₁FN₄O₃S
Color Off-white to yellow
SMILES

CC1=C2C(C=C(C(N[C@@H]3CCC[C@H](N4C[C@@H](N(S(=O)(C)=O)C)CC4)C3)=O)N2)=C(F)C=C1
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

Publications (4)

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Journal Impact Factor

Mol Cell

Chromatin-bound U2AF2 splicing factor ensures exon inclusion. [Abstract]

2025 May 15;85(10):1982-1998.e4. PMID: 40315850
Cancers (Basel)

Pharmacologic and Oncohistone Inhibition of SETD2 Converge on Genomic Instability. [Abstract]

2026 Mar 3;18(5):819. PMID: 41827754
bioRxiv

2025 July 15.
bioRxiv

2025 January 05.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (110.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2194 mL

11.0971 mL

22.1941 mL

5 mM

0.4439 mL

2.2194 mL

4.4388 mL

10 mM

0.2219 mL

1.1097 mL

2.2194 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 12.5 mg/mL (27.74 mM); Clear solution

This protocol yields a clear solution of ≥ 12.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (125.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

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

Solubility: ≥ 1.25 mg/mL (2.77 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

Protocol 3

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

Solubility: ≥ 1.25 mg/mL (2.77 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lampe JW, et al. Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies. ACS Med Chem Lett. 2021 Aug 24;12(10):1539-1545. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2194 mL	11.0971 mL	22.1941 mL	55.4853 mL
	5 mM	0.4439 mL	2.2194 mL	4.4388 mL	11.0971 mL
	10 mM	0.2219 mL	1.1097 mL	2.2194 mL	5.5485 mL
	15 mM	0.1480 mL	0.7398 mL	1.4796 mL	3.6990 mL
	20 mM	0.1110 mL	0.5549 mL	1.1097 mL	2.7743 mL
	25 mM	0.0888 mL	0.4439 mL	0.8878 mL	2.2194 mL
	30 mM	0.0740 mL	0.3699 mL	0.7398 mL	1.8495 mL
	40 mM	0.0555 mL	0.2774 mL	0.5549 mL	1.3871 mL
	50 mM	0.0444 mL	0.2219 mL	0.4439 mL	1.1097 mL
	60 mM	0.0370 mL	0.1850 mL	0.3699 mL	0.9248 mL
	80 mM	0.0277 mL	0.1387 mL	0.2774 mL	0.6936 mL
	100 mM	0.0222 mL	0.1110 mL	0.2219 mL	0.5549 mL

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EPZ-719

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) EPZ-719

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EPZ-719

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) EPZ-719

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EPZ-719 Related Classifications

HY-139626 Related Classifications