(R)-DNMDP
Based on 1 Customer Validation
(R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. (R)-DNMDP has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line.
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- Reinheit: 99.59%
- CAS. Nr.: 1630760-60-9
- Formel: C15H20N4O3
- Molecular Weight:304.34
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
3.8 nM
Compound: (R)-DNMDP
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Cytotoxicity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by Caspase-Glo reagent based assay
Cytotoxicity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by Caspase-Glo reagent based assay
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[PMID: 31749907] |
(R)-DNMDP (0.1 pM-1 mM; for 48 hours) has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line[1].
(S)-DNMDP has non-cytotoxic. Binding of PDE3A to the linker analogue is blocked by both trequinsin and (R)-DNMDP, but not by the (S)-DNMDP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1630760-60-9
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Appearance Solid
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Molecular Weight 304.34
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Formel C15H20N4O3
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Color Yellow to orange
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SMILES
O=C1C[C@@H](C)C(C2=CC=C(N(CC)CC)C([N+]([O-])=O)=C2)=NN1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (328.58 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (8.21 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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 (8.21 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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.
Reinheit & Dokumentation
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Data Sheet (272 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. de Waal L, et al. Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics. Nat Chem Biol. 2016 Feb;12(2):102-8. Nat Chem Biol. 2016 Feb;12(2):102-8. [Content Brief]
[2]. Luc DE WAAL, et al. Compositions and methods for cancer expressing pde3a or slfn12. WO2017027854A1.
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 | 3.2858 mL | 16.4290 mL | 32.8580 mL | 82.1450 mL |
| 5 mM | 0.6572 mL | 3.2858 mL | 6.5716 mL | 16.4290 mL | |
| 10 mM | 0.3286 mL | 1.6429 mL | 3.2858 mL | 8.2145 mL | |
| 15 mM | 0.2191 mL | 1.0953 mL | 2.1905 mL | 5.4763 mL | |
| 20 mM | 0.1643 mL | 0.8214 mL | 1.6429 mL | 4.1072 mL | |
| 25 mM | 0.1314 mL | 0.6572 mL | 1.3143 mL | 3.2858 mL | |
| 30 mM | 0.1095 mL | 0.5476 mL | 1.0953 mL | 2.7382 mL | |
| 40 mM | 0.0821 mL | 0.4107 mL | 0.8214 mL | 2.0536 mL | |
| 50 mM | 0.0657 mL | 0.3286 mL | 0.6572 mL | 1.6429 mL | |
| 60 mM | 0.0548 mL | 0.2738 mL | 0.5476 mL | 1.3691 mL | |
| 80 mM | 0.0411 mL | 0.2054 mL | 0.4107 mL | 1.0268 mL | |
| 100 mM | 0.0329 mL | 0.1643 mL | 0.3286 mL | 0.8214 mL |
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