1. Cell Cycle/DNA Damage
  2. DNA Alkylator/Crosslinker
  3. Treosulfan

Treosulfan  (Synonyms: NSC 39069; Treosulphan)

Cat. No.: HY-16503 Purity: ≥98.0%
COA Handling Instructions

Treosulfan (NSC 39069) is a bifunctional alkylating agent with activity in ovarian cancer and other solid tumor types.

For research use only. We do not sell to patients.

Treosulfan Chemical Structure

Treosulfan Chemical Structure

CAS No. : 299-75-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 77 In-stock
Solid
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10 mg USD 110 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Treosulfan (NSC 39069) is a bifunctional alkylating agent with activity in ovarian cancer and other solid tumor types.

IC50 & Target

DNA Alkylator[1]

In Vitro

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.

In Vivo

Treosulfan (1.5 g/kg/day) induces a rapid myeloablation, depletes the splenic B and T cells in mice. Treosulfan (1.5 g/kg/day) causes olny interleukin-2 production in spleen cells for a short time and without obvious significant effect on synthesis of tumor necrosis factor-α and/or IFN-γ in mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

278.30

Formula

C6H14O8S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]([C@@H](O)COS(C)(=O)=O)COS(C)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 16.67 mg/mL (59.90 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥98.0%

References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

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.

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Treosulfan Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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