2. Epigenetics
  3. Histone Methyltransferase
  4. EZM0414

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.

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

EZM0414 Chemical Structure

EZM0414 Chemical Structure

CAS No. : 2411748-50-8

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1 mg USD 340 In-stock
5 mg USD 850 In-stock
10 mg USD 1180 In-stock
25 mg USD 1750 In-stock
50 mg USD 2350 In-stock
100 mg USD 3150 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of EZM0414:

EZM0414 Related Antibodies

Top Publications Citing Use of Products

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

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[1].

IC50 & Target

SETD2/KMT3A

 

Cellular Effect
Cell Line Type Value Description References
KMS-11 IC50
370 nM
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.

EZM0414 Related Antibodies
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, 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.
Clinical Trial
Molecular Weight

400.49

Formula

C22H29FN4O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
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
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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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
Purity & Documentation
References

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.

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
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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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