CPUY074020
Based on 1 Customer Validation
CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.
For research use only. We do not sell to patients.
- Purity: 98.56%
- CAS No.: 902279-44-1
- Formula: C25H28N4O2
- Molecular Weight:416.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Histone Methyltransferase Isoforms
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Biological Activity
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EHMT2/G9a/KMT1C |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
3.18 μM
Compound: CPUY074020
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Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 72 hrs by MTT assay
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[PMID: 27720557] |
| HepG2 | IC50 |
7.93 μM
Compound: CPUY074020
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Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by MTT assay
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[PMID: 27720557] |
| MCF7 | IC50 |
4.52 μM
Compound: CPUY074020
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay
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[PMID: 27720557] |
CPUY074020 (2-8μM; 24 hours) induces cell death through apoptosis[1].
CPUY074020 (2.5-10μM ; 48 hours) dose-dependently de-regulates H3K9 trimethylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:2 μM, 4 μM, 8 μM
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Incubation Time:24 hours
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Result:Induced MCF-7 cells apoptosis.
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Cell Line:MCF-7 cells
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:48 hours
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Result:Dose-dependently de-regulated H3K9 trimethylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice
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Dosage:10 mg/kg
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Administration:Oral administration
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Result:t1/2=4.0 hours
Chemical Information
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CAS No. 902279-44-1
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Appearance Solid
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Molecular Weight 416.52
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Formula C25H28N4O2
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Color Brown to dark brown
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SMILES
O=C1C2=CC=CC=C2C3=C4C1=C(NCCN5CCCC5)C=C(N6CCCCC6)C4=NO3
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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 : 20 mg/mL (48.02 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: ≥ 2 mg/mL (4.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 (278 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 | 2.4008 mL | 12.0042 mL | 24.0085 mL | 60.0211 mL |
| 5 mM | 0.4802 mL | 2.4008 mL | 4.8017 mL | 12.0042 mL | |
| 10 mM | 0.2401 mL | 1.2004 mL | 2.4008 mL | 6.0021 mL | |
| 15 mM | 0.1601 mL | 0.8003 mL | 1.6006 mL | 4.0014 mL | |
| 20 mM | 0.1200 mL | 0.6002 mL | 1.2004 mL | 3.0011 mL | |
| 25 mM | 0.0960 mL | 0.4802 mL | 0.9603 mL | 2.4008 mL | |
| 30 mM | 0.0800 mL | 0.4001 mL | 0.8003 mL | 2.0007 mL | |
| 40 mM | 0.0600 mL | 0.3001 mL | 0.6002 mL | 1.5005 mL |