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Purity: ≥98%
Treosulfan (NSC 39069; Treosulphan) is a novel and potent DNA alkylating agent with activity in ovarian cancer and other solid tumor types. Treosulfan is the byproduct of an immunosuppressive, myeloablative, and antineoplastic bifunctional sulfonate alkylating agent. Treosulfan undergoes a nonenzymatic conversion to L-diepoxybutane via a monoepoxide intermediate in a physiological setting. DNA fragmentation and apoptosis are caused by the production of DNA interstrand crosslinks and alkylation of DNA at guanine residues by the monoepoxide intermediate and L-diepoxybutane. At higher dosages, this substance also exhibits myeloablative and immunosuppressive effects.
| Targets |
DNA Alkylator
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|---|---|
| ln Vitro |
Treosulfan is an agent that alkylates. Treosulfan exhibits nearly 100% cytotoxicity at 100 μg/mL on a number of cancer cell lines, including 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. When combined with LY 188011, treosulfan (0.1-100 μg/mL) shows increased activity against cancer cells. On the other hand, Treosulfan (1, 2.5, and 5 μg/ml) in combination with 5-FU (0.1, 0.25, and 0.5 μg/ml) exhibits antagonistic effects on Miapaca-2 cells at all doses and on Panc-1 cells at intermediate and high concentrations[1]. Treosulfan (800 µg/mL) significantly lowers erythrocyte forward scatter and raises the proportion of ROS, [Ca2+]i, and annexin-V-binding cells. When extracellular Ca2+ is removed, Treosulfan's effect on annexin-V binding is negated[2].
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| ln Vivo |
Treosulfan (1.5 g/kg/day) causes mice to rapidly undergo myeloablation and lose all of their splenic B and T cells. Treosulfan (1.5 g/kg/day) briefly increases the production of olny interleukin-2 in the spleen cells without clearly having a major impact on the synthesis of tumor necrosis factor-α and/or IFN-γ in mice[3].
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| Cell Assay |
In tissue culture plates with 96 wells, the cells are grown in 100 μL volume per well and plated at 1×104 cells/mL for cytotoxicity assays. After allowing the cells to adhere for a full night, they are cultured with varying concentrations of either Treosulfan alone or in conjunction with LY 188011. The drug combination is introduced either sequentially—the second drug is added 12 hours after the first—or simultaneously to the cell cultures. Alamar Blue® solution is added to the wells following a 72-hour incubation period before an additional overnight incubation. Next, absorbance is determined using a spectrophotometer, and drug cytotoxicity and cell proliferation are computed. Additionally, in certain experiments, trypan blue exclusion is used to determine proliferation and cytotoxicity, and an improved Neubauer hemocytometer is used to count cells. Cell viability is evaluated by staining the cells with 7-amino-actinomycin D (final concentration 200 μg/mL) and Annexin-V, followed by flow cytometry analysis using an FACS Scan flow cytometer[1].
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| Animal Protocol |
Mice: At 10 to 12 weeks of age, female BALB/c mice weighed about 20 g. Standard pelleted feed and unlimited water are provided to the animals. They are kept in a climate-controlled room with a 12-hour light/dark cycle. There are four groups that they are split up into: one group gets treated with liposomal NCI C01592 (37 mg/kg/day) for four days straight; another group receives NSC-26271 (0.1 g/kg/day) for two days straight; a control group does not receive any treatment. To sustain the animals' survival in the absence of bone marrow support, sublethal doses of NSC-26271, NCI C01592, and treosulfan are administered. Days 1, 3, 6, 9, and 12 following the final treatment dose are dedicated to animal sacrifice, during which the femurs and spleen are extracted. Two control and six treated animals are included at each time point [3].
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| References |
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| Molecular Formula |
C6H14O8S2
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|---|---|
| Molecular Weight |
278.30056
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| Exact Mass |
278.01
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| Elemental Analysis |
C, 25.89; H, 5.07; O, 45.99; S, 23.04
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| CAS # |
299-75-2
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| Related CAS # |
299-75-2 (Treosulfan); 55-98-1 (Busulfan); 52-24-4 (Thiotepa, Girostan; AI3-24916; NSC-6396)
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| Appearance |
Solid powder
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| SMILES |
CS(=O)(=O)OC[C@@H]([C@H](COS(=O)(=O)C)O)O
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| InChi Key |
YCPOZVAOBBQLRI-WDSKDSINSA-N
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| InChi Code |
InChI=1S/C6H14O8S2/c1-15(9,10)13-3-5(7)6(8)4-14-16(2,11)12/h5-8H,3-4H2,1-2H3/t5-,6-/m0/s1
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| Chemical Name |
[(2S,3S)-2,3-dihydroxy-4-methylsulfonyloxybutyl] methanesulfonate
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| Synonyms |
NSC-39069; Treosulfan; NSC 39069; NSC39069; (2S,3S)-2,3-Dihydroxybutane-1,4diyl dimethanesulfonate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~56 mg/mL (~201.2 mM)
Water: ~56 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 16.67 mg/mL (59.90 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5932 mL | 17.9662 mL | 35.9324 mL | |
| 5 mM | 0.7186 mL | 3.5932 mL | 7.1865 mL | |
| 10 mM | 0.3593 mL | 1.7966 mL | 3.5932 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05534620 | Not yet recruiting | Drug: Treosulfan Drug: Fludarabine |
Acute Myeloid Leukaemia (AML) Myelodysplastic Syndrome (MDS) |
medac GmbH | November 2023 | Phase 1 |
| NCT05807932 | Recruiting | Drug: Venetoclax Drug: Amsacrine |
Chronic Myelomonocytic Leukemia Myelodysplastic Syndromes |
Heinrich-Heine University, Duesseldorf |
June 26, 2023 | Phase 1 Phase 2 |
| NCT04965597 | Recruiting | Drug: Treosulfan Drug: Tacrolimus |
Hereditary Sideroblastic Anemia Bone Marrow Failure Syndrome |
Fred Hutchinson Cancer Center | April 19, 2022 | Phase 2 |
| NCT05636787 | Recruiting | Drug: Treosulfan Drug: Melphalan |
Multiple Myeloma | Insel Gruppe AG, University Hospital Bern |
June 6, 2023 | Phase 2 |
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