EZM0414 TFA
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 95.48%
- CAS 番号: 2411759-92-5
- 分子式: C24H30F4N4O4
- 分子量:514.51
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 EZM0414 TFA
More- Cell. 2026 Jun 11;189(12):3541-3552.e18. [Abstract]
- Cell Stem Cell. 2023 Apr 6;30(4):450-459.e9. [Abstract]
- Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
- Int J Biol Macromol. 2024 Oct 28:136767. [Abstract]
- Cell Rep. 2025 Jan 15;44(1):115219. [Abstract]
- Transl Psychiatry. 2026 Apr 1;16(1):275. [Abstract]
- Cancer Sci. 2026 May 22. [Abstract]
- Sci Rep. 2024 Jun 3;14(1):12728. [Abstract]
- Anim Reprod Sci. 2026 May 5;292:108229.
- Research Square Preprint. 2023 May 26.
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Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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SETD2/KMT3A |
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.
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Cell Line:multiple myeloma cells
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Concentration:
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Incubation Time:7 days
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Result:Inhibited cell proliferation.
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.
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Animal Model:KMS-11 Xenograft mouse models[3]
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Dosage:15-30 mg/kg
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Administration:po, twice a day for 35 days
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Result:Inhibited tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2411759-92-5
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性状 Solid
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分子量 514.51
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分子式 C24H30F4N4O4
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Color White to light yellow
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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
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別名
SETD2-IN-1 TFA
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell
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.
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Nat Chem Biol
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).
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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 -
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溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (281 KB)
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取扱説明書 (2659 KB)
参考文献
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 関連分類
HY-136328 関連分類
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