EPZ011989 trifluoroacetate
Based on 3 publication(s) in Google Scholar
EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers. EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- CAS No.: 1598383-41-5
- Formula: C37H52F3N5O6
- Molecular Weight:719.83
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) EPZ011989 trifluoroacetate
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
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EZH2 |
EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an Ki value of <3 nM[1].
EPZ-011989 trifluoroacetate reduces cellular H3K27 methylation with an IC50 value of 94 nM[1].
EPZ-011989 trifluoroacetate (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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CAS No. 1598383-41-5
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Appearance Solid
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Molecular Weight 719.83
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Formula C37H52F3N5O6
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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.O=C(O)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Solvent & Solubility
DMSO : 100 mg/mL (138.92 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (3.47 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 (3.47 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. * In solvent : -80°C, 6 months; -20°C, 1 month (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.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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). 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 | 1.3892 mL | 6.9461 mL | 13.8922 mL | 34.7304 mL |
| 5 mM | 0.2778 mL | 1.3892 mL | 2.7784 mL | 6.9461 mL | |
| 10 mM | 0.1389 mL | 0.6946 mL | 1.3892 mL | 3.4730 mL | |
| 15 mM | 0.0926 mL | 0.4631 mL | 0.9261 mL | 2.3154 mL | |
| 20 mM | 0.0695 mL | 0.3473 mL | 0.6946 mL | 1.7365 mL | |
| 25 mM | 0.0556 mL | 0.2778 mL | 0.5557 mL | 1.3892 mL | |
| 30 mM | 0.0463 mL | 0.2315 mL | 0.4631 mL | 1.1577 mL | |
| 40 mM | 0.0347 mL | 0.1737 mL | 0.3473 mL | 0.8683 mL | |
| 50 mM | 0.0278 mL | 0.1389 mL | 0.2778 mL | 0.6946 mL | |
| 60 mM | 0.0232 mL | 0.1158 mL | 0.2315 mL | 0.5788 mL | |
| 80 mM | 0.0174 mL | 0.0868 mL | 0.1737 mL | 0.4341 mL | |
| 100 mM | 0.0139 mL | 0.0695 mL | 0.1389 mL | 0.3473 mL |
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