Cat. No.: HY-136328

EZM0414 TFA

(Synonyms: SETD2-IN-1 TFA)

10 Cited Publications

Customer Review

Based on 10 publication(s) in Google Scholar

EZM0414 (SETD2-IN-1) TFA is the TFA salt form of EZM0414 (HY-144858). EZM0414 TFA is a potent, selective, orally active inhibitor of SETD2 (IC₅₀=18 nM in SETD2 biochemical assay; IC₅₀=34 nM in cellular assay). EZM0414 TFA can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.

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

Purity: 95.48%
CAS No.: 2411759-92-5
Formula: C₂₄H₃₀F₄N₄O₄
Molecular Weight:514.51

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

EZM0414 TFA Chemical Structure

CAS No.: 2411759-92-5

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

SETD2/KMT3A

All Histone Methyltransferase Isoforms :

In Vitro

EZM0414 inhibits proliferation of a panel of MM and DLBCL cell lines, withv of 0.24 μM for t(4;14) cell, 0.023 μM to >10 μM for DLBCL cell lines^[2].

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

Cell Proliferation Assay^[2]

Cell Line:

multiple myeloma cells
Concentration:
Incubation Time:

7 days
Result:

Inhibited cell proliferation.

In Vivo

In the t(4;14) MM cell line-derived xenograft model, KMS-11, EZM0414 shows robust tumor growth regressions. The antitumor effects observed correlated with reductions in intratumoral H3K36me3 levels demonstrating on-target inhibition of SETD2 methyltransferase activity in vivo^[2].
EZM0414 (15 和 30 mg/kg, p.o., twice a day for 35 days) inhibits tumor growth in NOD SCID mouse xenograft model implanted with human KMS-11 cells, and is well-tolerated^[3].
EZM0414 (50 mg/kg, p.o.) shows almost 100% oral bioavailability in rats and mice, t1/2 of 1.8 h (mice)and 3.8 h (rats)^[3].

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

Animal Model:

KMS-11 Xenograft mouse models^[3]
Dosage:

15-30 mg/kg
Administration:

po, twice a day for 35 days
Result:

Inhibited tumor growth.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2411759-92-5
Appearance Solid
Molecular Weight 514.51
Formula C₂₄H₃₀F₄N₄O₄
Color White to light yellow
SMILES

O=C(C(N1)=CC2=C1C(C)=CC=C2F)N[C@H]3C[C@@H](N4CCN(C(C)=O)CC4)CCC3.O=C(O)C(F)(F)F
Synonyms

SETD2-IN-1 TFA
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Publications (10)

All OthersCell Proliferation/Viability AssayWB

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Journal Impact Factor

Cell

p53 safeguards chemical reprogramming of human somatic cells toward pluripotency. [Abstract]

2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746
Cell Stem Cell

Highly efficient and rapid generation of human pluripotent stem cells by chemical reprogramming. [Abstract]

2023 Apr 6;30(4):450-459.e9. PMID: 36944335

EZM0414 TFA purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2023 Apr 6;30(4):450-459.e9. [Abstract]

Number of hCiPSC colonies induced from hASFs (hASFs-38040) (n = 3) and hADSCs (hADSCs-0618) (n = 4) with stage I condition (SI) or SI plus EZM0414 TFA (SET: 0.2 μM) using a three-stage protocol.
Nat Chem Biol

Drug addiction unveils a repressive methylation ceiling in EZH2-mutant lymphoma. [Abstract]

2023 Sep;19(9):1105-1115. PMID: 36973442

EZM0414 TFA purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]

Bar plots showing cell proliferation in the presence of EZM0414 TFA (SETD2-IN-1) at 0.1, 1, or 10 μM after 21-day treatment.

EZM0414 TFA purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]

Immunoblot showing H3K27me3 and H3K36me3 levels in lymphoma cell lines treated with 5 μM EZM0414 TFA (SETD2-IN-1) for 72 h.

EZM0414 TFA purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]

Immunoblot showing γH2AX and H3K36me3 levels in Karpas-422 treated with 5 μM EZM0414 TFA (SETD2-IN-1) for 10 days or 10 μM etoposide for 24 h.

EZM0414 TFA purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]

Aggregate profile plot of wild-type Karpas-422 H3K36me3 ChIP-Rx signal (y-axis) for EZM0414 TFA (SETD2-IN-1: 5 μM) treatment centered around H3K36me3 domains in wild-type cells (x-axis).
Int J Biol Macromol

SETD2 deficiency in peripheral sensory neurons induces allodynia by promoting NMDA receptor expression through NFAT5 in rodent models. [Abstract]

2024 Oct 28:136767. PMID: 39476923
Cell Rep

Menin orchestrates macrophage reprogramming to maintain the pulmonary immune homeostasis. [Abstract]

2025 Jan 15;44(1):115219. PMID: 39817905
Transl Psychiatry

Non-gene-edited neural stem cells reverse neuroinflammation and microbiota dysbiosis in a sprague-dawley rat model of autism spectrum disorder. [Abstract]

2026 Apr 1;16(1):275. PMID: 41922322
Cancer Sci

Blocking SETD2 Enhances the Therapeutic Efficiency of Menin Inhibitor in MLL-Fusion Leukemia. [Abstract]

2026 May 22. PMID: 42170936
Sci Rep

SPA inhibits hBMSC osteogenic differentiation and M1 macrophage polarization by suppressing SETD2 in acute suppurative osteomyelitis. [Abstract]

2024 Jun 3;14(1):12728. PMID: 38830934
Anim Reprod Sci

2026 May 5;292:108229.
Research Square Preprint

2023 May 26.

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (388.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 6.67 mg/mL (12.96 mM; ultrasonic and warming and heat to 60°C)

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

1.9436 mL

9.7180 mL

19.4360 mL

5 mM

0.3887 mL

1.9436 mL

3.8872 mL

10 mM

0.1944 mL

0.9718 mL

1.9436 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (9.72 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

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

Solubility: ≥ 5 mg/mL (9.72 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 5 mg/mL (9.72 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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 (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. John Lampe, et al. Substituted indoles and methods of use thereof. WO2020037079A1.

[2]. Jennifer Totman, et al. Pharmacologic Inhibition of the Histone Methyltransferase SETD2 with EZM0414 As a Novel Therapeutic Strategy in Relapsed or Refractory Multiple Myeloma and Diffuse Large B-Cell Lymphoma. Blood. Volume 138, Supplement 1, 23 November 2021, Page 1142.

[3]. Alford JS, et al. Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies. ACS Med Chem Lett. 2022 Jun 7;13(7):1137-1143 [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.9436 mL	9.7180 mL	19.4360 mL	48.5899 mL
	5 mM	0.3887 mL	1.9436 mL	3.8872 mL	9.7180 mL
	10 mM	0.1944 mL	0.9718 mL	1.9436 mL	4.8590 mL
DMSO	15 mM	0.1296 mL	0.6479 mL	1.2957 mL	3.2393 mL
	20 mM	0.0972 mL	0.4859 mL	0.9718 mL	2.4295 mL
	25 mM	0.0777 mL	0.3887 mL	0.7774 mL	1.9436 mL
	30 mM	0.0648 mL	0.3239 mL	0.6479 mL	1.6197 mL
	40 mM	0.0486 mL	0.2429 mL	0.4859 mL	1.2147 mL
	50 mM	0.0389 mL	0.1944 mL	0.3887 mL	0.9718 mL
	60 mM	0.0324 mL	0.1620 mL	0.3239 mL	0.8098 mL
	80 mM	0.0243 mL	0.1215 mL	0.2429 mL	0.6074 mL
	100 mM	0.0194 mL	0.0972 mL	0.1944 mL	0.4859 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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EZM0414 TFA

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) EZM0414 TFA

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (10)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EZM0414 TFA

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) EZM0414 TFA

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (10)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EZM0414 TFA Related Classifications

HY-136328 Related Classifications