Duocarmycin DM
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Duocarmycin DM, a DNA minor-groove alkylator, is an antibody agent conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity.
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- Pureté: 99.15%
- Formule: C28H27ClF3N3O5
- Masse moléculaire:577.98
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Daunorubicins/Doxorubicins |
The Duocarmycins and CC-1065 are members of a class of DNA minor groove, AT-sequence selective, and adenine-N3 alkylating agents, isolated from Streptomyces sp. that exhibit extremely potent cytotoxicity against the growth of cancer cells grown in culture[2].
Duocarmycin DM shows cytotoxicity to several human cancer cells, with IC50 of 22, 13.8, 3.87, 15.4, and 7.31 pM for HT-29, CL1-5, Caski, EJ, and LS174T, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Masse moléculaire 577.98
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Formule C28H27ClF3N3O5
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Color Off-white to light yellow
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SMILES
OC1=C2C(C=CC=C2)=C3C(N(C[C@H]3CCl)C(C4=CC5=C(N4)C=CC(OCCN(C)C)=C5)=O)=C1.OC(C(F)(F)F)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 100 mg/mL (173.02 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.33 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
[1]. Patil PC, et al. A Short Review on the Synthetic Strategies of Duocarmycin Analogs that are Powerful DNA Alkylating Agents. Anticancer Agents Med Chem. 2015;15(5):616-630. [Content Brief]
[2]. Koch MF, et al. Structural, Biochemical, and Computational Studies Reveal the Mechanism of Selective Aldehyde Dehydrogenase 1A1 Inhibition by Cytotoxic Duocarmycin Analogues. Angew Chem Int Ed Engl. 2015 Nov 9;54(46):13550-4. [Content Brief]
[3]. Chen KC, et al. Selective cancer therapy by extracellular activation of a highly potent glycosidic duocarmycin analogue. Mol Pharm. 2013;10(5):1773-1782. [Content Brief]
[4]. Tietze LF, Krewer B, von Hof JM, Frauendorf H, Schuberth I. Determination of the biological activity and structure activity relationships of drugs based on the highly cytotoxic duocarmycins and CC-1065. Toxins (Basel). 2009;1(2):134-150. [Content Brief]
[5]. Tietze LF, Schuster HJ, Schmuck K, Schuberth I, Alves F. Duocarmycin-based prodrugs for cancer prodrug monotherapy. Bioorg Med Chem. 2008;16(12):6312-6318. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.7302 mL | 8.6508 mL | 17.3016 mL | 43.2541 mL |
| 5 mM | 0.3460 mL | 1.7302 mL | 3.4603 mL | 8.6508 mL | |
| 10 mM | 0.1730 mL | 0.8651 mL | 1.7302 mL | 4.3254 mL | |
| 15 mM | 0.1153 mL | 0.5767 mL | 1.1534 mL | 2.8836 mL | |
| 20 mM | 0.0865 mL | 0.4325 mL | 0.8651 mL | 2.1627 mL | |
| 25 mM | 0.0692 mL | 0.3460 mL | 0.6921 mL | 1.7302 mL | |
| 30 mM | 0.0577 mL | 0.2884 mL | 0.5767 mL | 1.4418 mL | |
| 40 mM | 0.0433 mL | 0.2163 mL | 0.4325 mL | 1.0814 mL | |
| 50 mM | 0.0346 mL | 0.1730 mL | 0.3460 mL | 0.8651 mL | |
| 60 mM | 0.0288 mL | 0.1442 mL | 0.2884 mL | 0.7209 mL | |
| 80 mM | 0.0216 mL | 0.1081 mL | 0.2163 mL | 0.5407 mL | |
| 100 mM | 0.0173 mL | 0.0865 mL | 0.1730 mL | 0.4325 mL |
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