EZH2-IN-17
Based on 1 Customer Validation
EZH2-IN-17 (compound 28) is a potent and orally active EZH2 inhibitor with an IC50 value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively).
For research use only. We do not sell to patients.
- Purity: 98.08%
- CAS No.: 2489672-09-3
- Formula: C36H46N4O4
- Molecular Weight:598.77
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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
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All Histone Methyltransferase Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-422 | IC50 |
1.82 nM
Compound: 28
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Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant
Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant
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[PMID: 37956762] |
| Pfeiffer | IC50 |
1.73 nM
Compound: 28
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Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant
Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant
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[PMID: 37956762] |
| WSUDLCL2 | IC50 |
2.36 nM
Compound: 28
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Antiproliferative activity against human WSUDLCL2 cells harboring EZH2 Y641F mutant
Antiproliferative activity against human WSUDLCL2 cells harboring EZH2 Y641F mutant
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[PMID: 37956762] |
Chemical Information
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CAS No. 2489672-09-3
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Appearance Solid
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Molecular Weight 598.77
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Formula C36H46N4O4
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Color White to off-white
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SMILES
O=C1C(CNC(C2=CC(C3=CC=C(C(N4CCOCC4)CC5)C5=C3)=CC(N(C6CCOCC6)CC)=C2C)=O)=C(C)C=C(C)N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (167.01 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 (protect from light). 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 (protect from light). 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 (4.18 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 (4.18 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 (protect from light)
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 (273 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 (protect from 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 | 1.6701 mL | 8.3505 mL | 16.7009 mL | 41.7523 mL |
| 5 mM | 0.3340 mL | 1.6701 mL | 3.3402 mL | 8.3505 mL | |
| 10 mM | 0.1670 mL | 0.8350 mL | 1.6701 mL | 4.1752 mL | |
| 15 mM | 0.1113 mL | 0.5567 mL | 1.1134 mL | 2.7835 mL | |
| 20 mM | 0.0835 mL | 0.4175 mL | 0.8350 mL | 2.0876 mL | |
| 25 mM | 0.0668 mL | 0.3340 mL | 0.6680 mL | 1.6701 mL | |
| 30 mM | 0.0557 mL | 0.2783 mL | 0.5567 mL | 1.3917 mL | |
| 40 mM | 0.0418 mL | 0.2088 mL | 0.4175 mL | 1.0438 mL | |
| 50 mM | 0.0334 mL | 0.1670 mL | 0.3340 mL | 0.8350 mL | |
| 60 mM | 0.0278 mL | 0.1392 mL | 0.2783 mL | 0.6959 mL | |
| 80 mM | 0.0209 mL | 0.1044 mL | 0.2088 mL | 0.5219 mL | |
| 100 mM | 0.0167 mL | 0.0835 mL | 0.1670 mL | 0.4175 mL |
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