NUCC-0226272
Based on 1 Customer Validation
NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 3004503-12-9
- Formula: C67H91N9O8S
- Molecular Weight:1182.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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EZH2 |
NUCC-0226272 (0.01-10 μM; 5 days) shows anti-proliferative effect in LNCaP and 22Rv1 cells[1].
NUCC-0226272 (10 μM; 6 days) shows strong degradation of EZH2, as well as reduction of PRC2 component SUZ12, and reduced H3K27me3 levels in C4-2B cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| IP (4 mg/kg) | |
| Tmax (h) | 0.83 |
| Cmax (ng/mL) | 3650 |
| AUClast (min·ng/mL) | 12777389 |
| t1/2 (h) | 3.46 |
| CL (mL/min/kg) | 3.11 |
| Vss (L/kg) | 3.11 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3004503-12-9
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Appearance Solid
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Molecular Weight 1182.56
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Formula C67H91N9O8S
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Color White to off-white
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SMILES
CCN(C1CCOCC1)C2=CC(C3=CC=C(C=C3)CN4CCN(CC4)C(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O)=O)=CC(C(NCC8=C(C=C(NC8=O)C)C)=O)=C2C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (84.56 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. 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. 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: 3.5 mg/mL (2.96 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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.
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.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 0.8456 mL | 4.2281 mL | 8.4562 mL | 21.1406 mL |
| 5 mM | 0.1691 mL | 0.8456 mL | 1.6912 mL | 4.2281 mL | |
| 10 mM | 0.0846 mL | 0.4228 mL | 0.8456 mL | 2.1141 mL | |
| 15 mM | 0.0564 mL | 0.2819 mL | 0.5637 mL | 1.4094 mL | |
| 20 mM | 0.0423 mL | 0.2114 mL | 0.4228 mL | 1.0570 mL | |
| 25 mM | 0.0338 mL | 0.1691 mL | 0.3382 mL | 0.8456 mL | |
| 30 mM | 0.0282 mL | 0.1409 mL | 0.2819 mL | 0.7047 mL | |
| 40 mM | 0.0211 mL | 0.1057 mL | 0.2114 mL | 0.5285 mL | |
| 50 mM | 0.0169 mL | 0.0846 mL | 0.1691 mL | 0.4228 mL | |
| 60 mM | 0.0141 mL | 0.0705 mL | 0.1409 mL | 0.3523 mL | |
| 80 mM | 0.0106 mL | 0.0529 mL | 0.1057 mL | 0.2643 mL |