EPZ011989
Based on 3 publication(s) in Google Scholar
EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Pureza: 98.79%
- No. CAS: 1598383-40-4
- Fòrmula: C35H51N5O4
- Peso molecular:605.81
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Epigenetics Compound Library
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Histone Modification Research Compound Library
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Methylation Compound Library
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High-Throughput Bioactive Compound Library
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Posttranslational Modification Library
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Alkyne Compound Library
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Publications Citing Use of MedChemExpress (MCE) EPZ011989
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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EZH2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| WSUDLCL2 | IC50 |
385 nM
Compound: 8
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Antiproliferative activity against human WSUDLCL2 cells
Antiproliferative activity against human WSUDLCL2 cells
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[PMID: 35531606] |
EPZ011989 inhibits mutant and wild-type EZH2 with an Ki value of <3 nM[1].
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EPZ011989 reduces cellular H3K27 methylation with an IC50 value of 94 nM[1].
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EPZ011989 (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:WSU-DLCL2 cells
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Concentration:0-10 μM
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Incubation Time:11 days
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Result:Demonstrated an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice[1]
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Dosage:125, 250, 500, and 1000 mg/kg
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Administration:Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days
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Result:Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h.
Observed complete ablation of the methyl mark by the end of day 7.
Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time.
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Animal Model:Rat[1]
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Dosage:30, 100, and 300 mg/kg
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Administration:Oral, single
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Result:
dose (mg/kg) route t1/2 (h) tmax (h) Cmax (ng/mL) AUCinf (h*ng/mL) time above LCC (h) 30 p.o. 4.7 2 240 970 4 100 p.o. 3.9 2.7 1600 5600 8 300 p.o. 3.7 2.7 2900 10000 10
Chemical Information
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No. CAS 1598383-40-4
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Appearance Solid
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Peso molecular 605.81
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Fòrmula C35H51N5O4
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Color Light yellow to yellow
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SMILES
O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#CCN3CCOCC3)=CC(N(CC)[C@H]4CC[C@H](N(CCOC)C)CC4)=C2C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Immunother Cancer
Druggable epigenetic suppression of interferon-induced chemokine expression linked to MYCN amplification in neuroblastoma. [Abstract]2021 May;9(5):e001335. PMID: 34016720 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431
Solvente y solubilidad
DMSO : 100 mg/mL (165.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (4.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6507 mL | 8.2534 mL | 16.5068 mL | 41.2671 mL |
| 5 mM | 0.3301 mL | 1.6507 mL | 3.3014 mL | 8.2534 mL | |
| 10 mM | 0.1651 mL | 0.8253 mL | 1.6507 mL | 4.1267 mL | |
| 15 mM | 0.1100 mL | 0.5502 mL | 1.1005 mL | 2.7511 mL | |
| 20 mM | 0.0825 mL | 0.4127 mL | 0.8253 mL | 2.0634 mL | |
| 25 mM | 0.0660 mL | 0.3301 mL | 0.6603 mL | 1.6507 mL | |
| 30 mM | 0.0550 mL | 0.2751 mL | 0.5502 mL | 1.3756 mL | |
| 40 mM | 0.0413 mL | 0.2063 mL | 0.4127 mL | 1.0317 mL | |
| 50 mM | 0.0330 mL | 0.1651 mL | 0.3301 mL | 0.8253 mL | |
| 60 mM | 0.0275 mL | 0.1376 mL | 0.2751 mL | 0.6878 mL | |
| 80 mM | 0.0206 mL | 0.1032 mL | 0.2063 mL | 0.5158 mL | |
| 100 mM | 0.0165 mL | 0.0825 mL | 0.1651 mL | 0.4127 mL |
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