EZM0414

Name: EZM0414
Brand: MedChemExpress
SKU: HY-144858
Rating: 5.0 (6 reviews)

Cat. No.: HY-144858 Pureza: 99.11%: Ficha de datos
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EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC₅₀=18 nM in SETD2 biochemical assay; IC₅₀=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 2411748-50-8

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Revisión del cliente

Based on 6 publication(s) in Google Scholar

Other Forms of EZM0414:

EZM0414 TFA In-stock

6 Publications Citing Use of MCE EZM0414

Others

Cell Proliferation/Viability Assay

: EZM0414 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 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 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 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 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).

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Histone Methyltransferase:

Ver todas las isoformas

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

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

SETD2/KMT3A

Cellular Effect

Cell Line	Type	Value	Description	References
KMS-11	IC₅₀	370 1 Compound: EZM0414	Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by CellTiter-glo luminescence assay Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by CellTiter-glo luminescence assay	[PMID: 35859865]
KMS-11	IC₅₀	370 1 Compound: EZM0414	Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by CellTiter-glo luminescence assay Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by CellTiter-glo luminescence assay	[PMID: 35859865]
KMS-11	IC₅₀	370 1 Compound: EZM0414	Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by CellTiter-glo luminescence assay Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability incubated for 14 days by CellTiter-glo luminescence assay	[PMID: 35859865]

In Vitro

EZM0414 inhibits proliferation of a panel of MM and DLBCL cell lines, with IC₅₀s of 0.24 μM for t(4;14) cell, 0.023 μM- >10 μM for DLBCL cell lines^[2].

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

In Vivo

EZM0414 (15 and 30 mg/kg, p.o., BID, daily, ) 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, t_1/2 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.

Peso molecular

400.49

Fòrmula

C₂₂H₂₉FN₄O₂

No. CAS

2411748-50-8

Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=C2C(NC(C(N[C@H]3C[C@](N4CCN(CC4)C(C)=O)([H])CCC3)=O)=C2)=C(C=C1)C

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, sealed storage, away from moisture and light

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

Solvente y solubilidad

In Vitro:

DMSO : 120 mg/mL (299.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4969 mL	12.4847 mL	24.9694 mL
5 mM	0.4994 mL	2.4969 mL	4.9939 mL
10 mM	0.2497 mL	1.2485 mL	2.4969 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad
Calculadora de dilución

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

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Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Calculation results:

Working solution concentration: mg/mL

Pureza y Documentación

Purity: 99.11%

Select Batch:

Ficha de datos (275 KB) SDS (252 KB)

COA (250 KB) HNMR (233 KB) CNMR (269 KB) LCMS (88 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. 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.

[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

DMSO	1 mM	2.4969 mL	12.4847 mL	24.9694 mL	62.4235 mL
	5 mM	0.4994 mL	2.4969 mL	4.9939 mL	12.4847 mL
	10 mM	0.2497 mL	1.2485 mL	2.4969 mL	6.2424 mL
	15 mM	0.1665 mL	0.8323 mL	1.6646 mL	4.1616 mL
	20 mM	0.1248 mL	0.6242 mL	1.2485 mL	3.1212 mL
	25 mM	0.0999 mL	0.4994 mL	0.9988 mL	2.4969 mL
	30 mM	0.0832 mL	0.4162 mL	0.8323 mL	2.0808 mL
	40 mM	0.0624 mL	0.3121 mL	0.6242 mL	1.5606 mL
	50 mM	0.0499 mL	0.2497 mL	0.4994 mL	1.2485 mL
	60 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0404 mL
	80 mM	0.0312 mL	0.1561 mL	0.3121 mL	0.7803 mL
	100 mM	0.0250 mL	0.1248 mL	0.2497 mL	0.6242 mL

EZM0414 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:

EZM04142411748-50-8EZM 0414EZM-0414Histone Methyltransferaserelapsed or refractory multiple myelomadiffuse large B-cell lymphomaSETD2oralDLBCLInhibitorinhibitorinhibit

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EZM0414

Revisión del cliente

Other Forms of EZM0414:

EZM0414 Related Antibodies

6 Publications Citing Use of MCE EZM0414

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Histone Methyltransferase:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

EZM0414 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

EZM0414 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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SAFETY DATA SHEET (SDS)

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