MC3817
Based on 1 Customer Validation
MC3817 is a selective DNMT1 inhibitor. MC3817 inhibits DNMT1 and DNMT3A/3L with IC50s of 0.044 μM and > 10μM, respectively. MC3817 inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage MC3817 elevates cleaved Caspase 3, P53, and γH2AX. MC3817 can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.88%
- Fòrmula: C33H41Cl4N9O
- Peso molecular:721.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Actividad biológica
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DNMT1 0.044 μM (IC50) |
MC3817 (compound 14) (0.05-100 μM, 48 h) exhibits antiproliferative activity against A549 and H460 (non-small cell and lung cancer), HCT-116 (colon cancer), HeLa (cervical cancer), MDA-MB-231 (triple-negative breast cancer), and U937 (histiocytic lymphoma) cells[1].
MC3817 (2 μM, 24 and 48 h) induces S/G2M phase arrest and triggers apoptotic cell death in HCT-116 cells[1].
MC3817 (0.5-5 μM, 16-48 h) triggers DNA damage and activates the p53/γH2AX pathway, leading to cell-cycle arrest and apoptosis in HCT 116 cells[1].
MC3817 (2.5 μM, 48 h) induces a much higher level of apoptosis in HCT-116 P53 WT cells compared with HCT-116 P53−/− cells [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 , H460, HCT-116, HeLa , MDA-MB 231, and U937
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Concentration:0.05-100 μM
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Incubation Time:48 h
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Result:Had IC50 of 5.5 μM, 6.8 μM, 0.4 μM, 4.2 μM, 1.9 μM and 5.5μM for A549 cells, H460 cells, HCT-116 cells, HeLa cells, MDA-MB 231 cells, and U937 cells.
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Cell Line:HCT-116 cells
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Concentration:2 μM
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Incubation Time:48 h
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Result:Caused a block in the S/G2M phase associated with apoptotic cell death, affecting over 50% of the cells after 48 h.
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Cell Line:HCT-116 cells
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Concentration:0.5, 1, 2.5, 5 μM
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Incubation Time:48 h
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Result:Induced the accumulation of γH2AX and elevated p53 levels, indicating p53 stabilization and activation in response to DNA damage.
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Cell Line:HCT-116 P53−/− cells and HCT-116 P53 WT cells.
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Concentration:2.5 μM
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Incubation Time:48 h
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Result:Induced apoptotic cell death, as evidenced by significant PI/Annexin V fluorescence and extensive membrane blebbing in both cell lines.
Chemical Information
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Appearance Solid
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Peso molecular 721.55
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Fòrmula C33H41Cl4N9O
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC(CN(C)C)=CC(NC2=NC(N)=NC(C)=C2)=C1)C3=CC(CN(C)C)=CC(NC4=C5C=CC=CC5=NC=C4)=C3.Cl.Cl.Cl.Cl
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (138.59 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: ≥ 2.5 mg/mL (3.46 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 (3.46 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 (277 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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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, 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 |
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| DMSO | 1 mM | 1.3859 mL | 6.9295 mL | 13.8591 mL | 34.6476 mL |
| 5 mM | 0.2772 mL | 1.3859 mL | 2.7718 mL | 6.9295 mL | |
| 10 mM | 0.1386 mL | 0.6930 mL | 1.3859 mL | 3.4648 mL | |
| 15 mM | 0.0924 mL | 0.4620 mL | 0.9239 mL | 2.3098 mL | |
| 20 mM | 0.0693 mL | 0.3465 mL | 0.6930 mL | 1.7324 mL | |
| 25 mM | 0.0554 mL | 0.2772 mL | 0.5544 mL | 1.3859 mL | |
| 30 mM | 0.0462 mL | 0.2310 mL | 0.4620 mL | 1.1549 mL | |
| 40 mM | 0.0346 mL | 0.1732 mL | 0.3465 mL | 0.8662 mL | |
| 50 mM | 0.0277 mL | 0.1386 mL | 0.2772 mL | 0.6930 mL | |
| 60 mM | 0.0231 mL | 0.1155 mL | 0.2310 mL | 0.5775 mL | |
| 80 mM | 0.0173 mL | 0.0866 mL | 0.1732 mL | 0.4331 mL | |
| 100 mM | 0.0139 mL | 0.0693 mL | 0.1386 mL | 0.3465 mL |
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