EZM0414 TFA (Synonyms: SETD2-IN-1 TFA)

Name: EZM0414 TFA
Brand: MedChemExpress
SKU: HY-136328
Rating: 5.0 (6 reviews)

Cat. No.: HY-136328 Purity: 95.48%: Data Sheet
COA

SDS
Handling Instructions
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Technical Support

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.

CAS No. : 2411759-92-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of EZM0414 TFA:

EZM0414 In-stock

6 Publications Citing Use of MCE EZM0414 TFA

Others

Cell Proliferation/Viability Assay

: 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.

: 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).

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View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

SETD2/KMT3A

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

Molecular Weight

514.51

Formula

C₂₄H₃₀F₄N₄O₄

CAS No.

2411759-92-5

Appearance

Solid

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

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)

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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
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: ≥ 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.
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: ≥ 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.
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: ≥ 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

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, 2 years; -20°C, 1 year (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: 97.20%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (253 KB) HNMR (139 KB) RP-HPLC (245 KB) LCMS (95 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]

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.

EZM0414 TFA 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.

Keywords:

EZM04142411759-92-5SETD2-IN-1EZM 0414EZM-0414Histone MethyltransferasecancerSETD2histonemethyltransferasesInhibitorinhibitorinhibit

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EZM0414 TFA (Synonyms: SETD2-IN-1 TFA)

Customer Review

Other Forms of EZM0414 TFA:

EZM0414 TFA Related Antibodies

6 Publications Citing Use of MCE EZM0414 TFA

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

EZM0414 TFA Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

EZM0414 TFA Related Classifications

Keywords:

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Customer Review

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