| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Thiotepa or Thio-TEPA (NSC-6396; AI3 24916; WR45312; Girostan), an approved drug for cancer treatment, is a potent DNA alkylating agent with antitumor activity. Thiotepa is a polyfunctional, organophosphorus alkylating agent and a stable derivative of N,N',N''-triethylenephosphoramide (TEPA), with antineoplastic activity. Upon administration, thiotepa is converted into highly reactive ethylenimine groups, which covalently bind to nucleophilic groups in DNA and demonstrate a preference for the N7 position of guanine bases. This induces crosslinking of alkylated guanine bases in double-stranded DNA, interferes with both DNA replication and cell division, and results in both the induction of apoptosis and the inhibition of cell growth.
| Targets |
DNA Alkylator
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|---|---|
| ln Vitro |
After being incubated, rat liver slices show alkylating activity for thio-TEPA. At all doses of 2, 5, and 10 mM, thio-TEPA does not accumulate in rat liver slices and has no effect on their viability[1].
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| ln Vivo |
During the first 10 weeks, donor-type blood chimerism is enhanced by thio-TEPA (20 mg/kg, i.p.) combined with total body irradiation (TBI), but it is not significantly higher than that of the TBI group alone. In mice, thio-TEPA alone enhances engraftment over the short and long terms[2].
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| References |
| Molecular Formula |
C6H12N3PS
|
|---|---|
| Molecular Weight |
189.2183
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| Exact Mass |
189.05
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| Elemental Analysis |
C, 38.09; H, 6.39; N, 22.21; P, 16.37; S, 16.95
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| CAS # |
52-24-4
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| Related CAS # |
55-98-1 (Busulfan); 299-75-2 (Treosulfan)
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| Appearance |
Solid powder
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| SMILES |
S=P(N1CC1)(N2CC2)N3CC3
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| InChi Key |
FOCVUCIESVLUNU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H12N3PS/c11-10(7-1-2-7,8-3-4-8)9-5-6-9/h1-6H2
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| Chemical Name |
tri(aziridin-1-yl)phosphine sulfide
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| Synonyms |
NSC-6396; AI3 24916; WR45312; NSC 6396; AI324916; WR 45312; NSC6396; AI3-24916; Girostan; thiophosphoramide; thiophosphamide; triethylene thiophosphoramide. trade names: Girostan; STEPA; TESPA; Thiofozil; Thioplex; Tifosyl. Foreign brand names: Ledertepa; Oncotiotepa; Onco Tiotepa; Tespamin; Tespamine; Thiotef; TioTEF; TSPA; WR45312.
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 50~100 mg/mL ( 264.24 ~528.48 mM )
Water : ~100 mg/mL Ethanol : ~100 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (13.21 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (13.21 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (13.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2849 mL | 26.4243 mL | 52.8485 mL | |
| 5 mM | 1.0570 mL | 5.2849 mL | 10.5697 mL | |
| 10 mM | 0.5285 mL | 2.6424 mL | 5.2849 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.
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