DMU2105
Based on 1 Customer Validation
DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.31%
- No. CAS: 1821143-79-6
- Fòrmula: C18H13NO
- Peso molecular:259.31
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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CYP1B1 10 nM (IC50) |
CYP1A1 742 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
1 μM
Compound: 7k; DMU2105
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Inhibition of human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 0.02 uM by MTT assay (Rvb = 61 +/- 8 uM)
Inhibition of human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 0.02 uM by MTT assay (Rvb = 61 +/- 8 uM)
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[PMID: 28222316] |
| HEK293 | EC50 |
8.5 μM
Compound: 7k; DMU2105
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Potentiation of cisplatin-induced cytotoxicity against HEK293 cells by measuring cisplatin EC50 at 10 times CYP1B1 inhibitory IC50 by MTT assay (Rvb = 8.7 +/- 0.7 uM)
Potentiation of cisplatin-induced cytotoxicity against HEK293 cells by measuring cisplatin EC50 at 10 times CYP1B1 inhibitory IC50 by MTT assay (Rvb = 8.7 +/- 0.7 uM)
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[PMID: 28222316] |
| HEK293 | IC50 |
0.004 μM
Compound: 7k; DMU2105
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Inhibition of human liver CYP1B1 expressed in HEK293 cells using CEC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
Inhibition of human liver CYP1B1 expressed in HEK293 cells using CEC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
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[PMID: 28222316] |
| HEK293 | IC50 |
0.053 μM
Compound: 7k; DMU2105
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Inhibition of human liver CYP1B1 expressed in HEK293 cells using 7-ethoxyresorufin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
Inhibition of human liver CYP1B1 expressed in HEK293 cells using 7-ethoxyresorufin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
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[PMID: 28222316] |
DMU2105 (Compound 7k) shows 74 and 120-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of DMU2105 however, the EC50 goes down to 1 μM indicating that the cells have suffered from toxicity which may have been mediated by CYP1B1 inhibition. Un-transfected cells (HEK293: pcDNA3.1), when treated with cisplatin and DMU2105 (10×IC50) do not show any perceptible decrease of cisplatin EC50 (8.5 μM ± 0.9)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1821143-79-6
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Appearance Solid
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Peso molecular 259.31
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Fòrmula C18H13NO
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=CN=C1)/C=C/C2=CC=C3C=CC=CC3=C2
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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 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 33.33 mg/mL (128.53 mM; ultrasonic and warming and heat to 60°C; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: 2.67 mg/mL (10.30 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.67 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 (26.7 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.
Pureza y Documentación
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Ficha de datos (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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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8564 mL | 19.2819 mL | 38.5639 mL | 96.4097 mL |
| 5 mM | 0.7713 mL | 3.8564 mL | 7.7128 mL | 19.2819 mL | |
| 10 mM | 0.3856 mL | 1.9282 mL | 3.8564 mL | 9.6410 mL | |
| 15 mM | 0.2571 mL | 1.2855 mL | 2.5709 mL | 6.4273 mL | |
| 20 mM | 0.1928 mL | 0.9641 mL | 1.9282 mL | 4.8205 mL | |
| 25 mM | 0.1543 mL | 0.7713 mL | 1.5426 mL | 3.8564 mL | |
| 30 mM | 0.1285 mL | 0.6427 mL | 1.2855 mL | 3.2137 mL | |
| 40 mM | 0.0964 mL | 0.4820 mL | 0.9641 mL | 2.4102 mL | |
| 50 mM | 0.0771 mL | 0.3856 mL | 0.7713 mL | 1.9282 mL | |
| 60 mM | 0.0643 mL | 0.3214 mL | 0.6427 mL | 1.6068 mL | |
| 80 mM | 0.0482 mL | 0.2410 mL | 0.4820 mL | 1.2051 mL | |
| 100 mM | 0.0386 mL | 0.1928 mL | 0.3856 mL | 0.9641 mL |
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