Treosulfan
Based on 3 publication(s) in Google Scholar
Treosulfan (NSC 39069) is a bifunctional alkylating agent with activity in ovarian cancer and other solid tumor types.
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- Pureza: 98.0%
- No. CAS: 299-75-2
- Fòrmula: C6H14O8S2
- Peso molecular:278.30
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) Treosulfan
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Actividad biológica
DNA Alkylator[1]
Treosulfan is an alkylating agent. Treosulfan inhibits several cancer cell lines, such as Panc-1, Miapaca-2 and Capan-2 cells, with IC50s of 3.6 μg/mL, 1.8 μg/mL and 2.1 μg/mL respectively, and shows nearly 100% cytotoxicity on these cell lines at 100 μg/mL. Treosulfan (0.1-100 μg/mL) in combination with LY 188011 exhibits enhanced activity against cancer cells. However, Treosulfan (1, 2.5, 5 μg/ml) combined with 5-FU (0.1, 0.25, 0.5 μg/ml) has antagonistic effect on Panc-1 cells at intermediate and high concentrations, and on Miapaca-2 cells at all doses[1]. Treosulfan (800 μg/mL) dramatically reduces erythrocyte forward scatter, increases the percentage of annexin-V-binding cells, [Ca2+]i, and ROS. Removal of extracellular Ca2+ abrogates the effect of Treosulfan on annexin-V-binding[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 299-75-2
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Appearance Solid
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Peso molecular 278.30
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Fòrmula C6H14O8S2
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Color White to off-white
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SMILES
O[C@H]([C@@H](O)COS(C)(=O)=O)COS(C)(=O)=O
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Synonyms
NSC 39069; Treosulphan
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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
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
CNS-wide repopulation by hematopoietic-derived microglia-like cells corrects progranulin deficiency in mice. [Abstract]2024 Jul 5;15(1):5654. PMID: 38969669 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Res Sq
CNS Repopulation by Hematopoietic-Derived Microglia-Like Cells Corrects Progranulin deficiency. [Abstract]2023 Sep 12:rs.3.rs-3263412. PMID: 37790525
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (359.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (179.66 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (8.98 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 (8.98 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 16.67 mg/mL (59.90 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocolo
For cytotoxicity assays, the cells are plated at 1×104 cells/mL grown in 100 μL volume per well of 96-well tissue culture plates. The cells are left to adhere overnight and thereafter incubated with different concentrations of Treosulfan alone or in combination with LY 188011. The drug combination is added to the cell cultures simultaneously or sequentially (the second drug added 12 h after the first). After 72 h of incubation, Alamar Blue® solution is added to the wells prior to further overnight incubation. Absorbance is then measured on a spectrophotometer and cell proliferation and cytotoxicity of drugs are calculated. In some experiments, proliferation and cytotoxicity are also determined by using trypan blue exclusion and cell counting with an improved Neubauer hemocytometer and cell viability assessed by staining the cells with 7-amino-actinomycin D (final concentration 200 μg/mL) and Annexin-V and analyzing via flow cytometry using a FACS Scan flow cytometer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Female BALB/c mice are 10 to 12 weeks old and weighed approximately 20 g. Animals are fed with standard pelleted food and water ad libitum. They are housed in a climatized chamber with a dark/light cycle of 12 hours. They are divided into four groups: one group is given Treosulfan (1.5 g/kg/day) for 3 consecutive days, one group receives NSC-26271 (0.1 g/kg/day) for 2 consecutive days, one group is treated with liposomal NCI C01592 (37 mg/kg/day) for 4 consecutive days, and there is a control group with no treatment. NSC-26271, NCI C01592, and Treosulfan doses are given at sublethal doses to maintain survival of the animals without bone marrow support. Animals are sacrificed on days 1, 3, 6, 9, and 12, after the last dose of treatment, and the spleen and femurs are removed. Six animals are included in each time point for the treated animals and two control animals[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Nitsch E, et al. Synergistic cytotoxic activity of treosulfan and LY 188011 in pancreatic cancer cell lines. Anticancer Res. 2014 Apr;34(4):1779-84. [Content Brief]
[2]. Peter T, et al. Programmed erythrocyte death following in vitro Treosulfan treatment. Cell Physiol Biochem. 2015;35(4):1372-80. [Content Brief]
[3]. Sjöö F, et al. Myeloablative and immunosuppressive properties of treosulfan in mice. Exp Hematol. 2006 Jan;34(1):115-21. [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. 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.5932 mL | 17.9662 mL | 35.9324 mL | 89.8311 mL |
| 5 mM | 0.7186 mL | 3.5932 mL | 7.1865 mL | 17.9662 mL | |
| 10 mM | 0.3593 mL | 1.7966 mL | 3.5932 mL | 8.9831 mL | |
| 15 mM | 0.2395 mL | 1.1977 mL | 2.3955 mL | 5.9887 mL | |
| 20 mM | 0.1797 mL | 0.8983 mL | 1.7966 mL | 4.4916 mL | |
| 25 mM | 0.1437 mL | 0.7186 mL | 1.4373 mL | 3.5932 mL | |
| 30 mM | 0.1198 mL | 0.5989 mL | 1.1977 mL | 2.9944 mL | |
| 40 mM | 0.0898 mL | 0.4492 mL | 0.8983 mL | 2.2458 mL | |
| 50 mM | 0.0719 mL | 0.3593 mL | 0.7186 mL | 1.7966 mL | |
| 60 mM | 0.0599 mL | 0.2994 mL | 0.5989 mL | 1.4972 mL | |
| 80 mM | 0.0449 mL | 0.2246 mL | 0.4492 mL | 1.1229 mL | |
| 100 mM | 0.0359 mL | 0.1797 mL | 0.3593 mL | 0.8983 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Treosulfan Related Classifications
HY-16503 Related Classifications
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