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Thio-TEPA

Name: Thio-TEPA
Brand: TargetMol
SKU: T1250
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1250Cas No. 52-24-4

Alias Triethylenethiophosphoramide, Tiofosyl, Tiofosfamid

Thio-TEPA (Tiofosyl) is a polyfunctional, organophosphorus alkylating agent with antineoplastic activity.

Thio-TEPA

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Purity: 99.07%

Catalog No. T1250Alias Triethylenethiophosphoramide, Tiofosyl, TiofosfamidCas No. 52-24-4

Thio-TEPA (Tiofosyl) is a polyfunctional, organophosphorus alkylating agent with antineoplastic activity.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$31	In Stock	In Stock
10 mg	$44	In Stock	In Stock
25 mg	$72	In Stock	In Stock
50 mg	$113	In Stock	In Stock
100 mg	$189	In Stock	In Stock
200 mg	$278	In Stock	In Stock
500 mg	$475	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$79	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.07%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Thio-TEPA AI Summary

Thio-TEPA demonstrates a wide range of bioactivities and pharmacokinetic properties suggestive of its potential as a therapeutic agent. In in vivo studies, it exhibits significant antineoplastic effects, particularly against P388 leukemia and L1210 leukemia in CD2F1 male mice, with an increase in life span (ILS) of up to 141.0% and a T/C ratio of 155.0%. It has an optimal dosing of 6 mg/kg/day and showcases a therapeutic ratio of 2.75 and LD50 of 18.0 mg/kg. The compound has shown activity in additional cancer models, including cytotoxic effects against various human tumor cell lines such as breast, renal, non-small cell lung, leukemia, melanoma, central nervous system, prostate, and colon cell lines, with IC50 values ranging from 1400.0 nM to 6970.0 nM. Pharmacokinetically, Thio-TEPA has a total body clearance rate of 6.7 mL/min/kg and a renal clearance of 0.03 mL/min/kg in humans. It also exhibits a volume of distribution at steady state of 1.6 L/kg and a half-life of 2.7 hours. Mechanistically, Thio-TEPA inhibits various enzymes and transporters, including human cytochrome P450 2B6, rat cytochrome P450 2B1, and human liver OATP transporters, showing varying degrees of inhibition. It also shows a high partition ratio in both human and rat cytochrome P450 2B6. Additionally, it has demonstrated inhibitory activity against human BSEP with an IC50 value greater than 135000.0 nM and antiviral activity against SARS-CoV-2 by reducing induced cytotoxicity of virus-exposed cells. Furthermore, Thio-TEPA indicates liver toxicity in humans and moderate to severe hepatotoxicity in preclinical models. It has been associated with a drug-induced liver injury severity class index of 3.0 and various levels of specific liver toxicities. In summary, Thio-TEPA is a multi-faceted therapeutic agent with significant antitumor, enzyme inhibition, transporter inhibition, and potential antiviral activities, along with notable pharmacokinetic and hepatotoxic profiles..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Thio-TEPA (Tiofosyl) is a polyfunctional, organophosphorus alkylating agent with antineoplastic activity.
Synonyms	Triethylenethiophosphoramide, Tiofosyl, Tiofosfamid

Chemical Properties

Molecular Weight	189.22
Formula	C₆H₁₂N₃PS
Cas No.	52-24-4
Smiles	P(=S)(N1CC1)(N2CC2)N3CC3
Relative Density.	1.5g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 91 mg/mL (480.92 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 3.3 mg/mL (17.44 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	5.2849 mL	26.4243 mL	52.8485 mL	264.2427 mL
5 mM	1.0570 mL	5.2849 mL	10.5697 mL	52.8485 mL
10 mM	0.5285 mL	2.6424 mL	5.2849 mL	26.4243 mL
20 mM	0.2642 mL	1.3212 mL	2.6424 mL	13.2121 mL
50 mM	0.1057 mL	0.5285 mL	1.0570 mL	5.2849 mL
100 mM	0.0528 mL	0.2642 mL	0.5285 mL	2.6424 mL

Calculator

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc