| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Mitotane-13C6 is the ¹³C-labeled version of Mitotane, which is an isomer of DDD and a derivative of dichlorodiphenyltrichloroethane (DDT). Mitotane targets adrenocortical carcinoma primarily through lipotoxicity resulting from the accumulation of intracellular free cholesterol. It also inhibits adrenal steroidogenesis and modifies lipid metabolism.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
The in vitro activity of Mitotane-13C6 mirrors that of its non-labeled parent compound, Mitotane, which exhibits significant biological activity in inhibiting adrenal steroidogenesis and modifying lipid metabolism. Mitotane-13C6 is used as an internal standard in in vitro assays to accurately quantify the concentration of Mitotane. |
| ln Vivo |
In vivo, Mitotane-13C6 is used as a tracer to study the pharmacokinetics and metabolism of Mitotane. Mitotane exerts its adrenocortical effects at least in part through lipotoxicity resulting from the accumulation of intracellular free cholesterol. The ¹³C-labeled version allows for precise tracking of the drug's distribution and metabolism in animal models.
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| Enzyme Assay |
The primary application of Mitotane-13C6 is as an internal standard in analytical chemistry. In a typical LC-MS/MS workflow, a known amount of the labeled compound is added to the biological sample (e.g., plasma or tissue homogenate). Following extraction, the sample is analyzed by LC-MS/MS. The internal standard corrects for variability in the analytical process, enabling accurate quantification of the non-labeled Mitotane.
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| Cell Assay |
In cellular assays, Mitotane-13C6 is used to quantify the intracellular concentration of Mitotane. Cells are treated with Mitotane, and the internal standard is added to the cell lysates before LC-MS/MS analysis. This allows researchers to accurately measure drug uptake and accumulation in cell lines.
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| Animal Protocol |
In animal studies, Mitotane-13C6 is utilized as an internal standard for the quantification of Mitotane in pharmacokinetic studies. Following administration to animal models, blood or tissue samples are collected at various time points. The labeled internal standard is added to these samples before LC-MS/MS analysis.
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| ADME/Pharmacokinetics |
As a ¹³C-labeled compound, Mitotane-13C6 has a distinct mass shift (typically +6 Da) that allows for its use as an internal standard. It is chemically stable and can be stored as a solid powder. Its molecular weight is 326.00.
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| Toxicity/Toxicokinetics |
Mitotane-13C6 is intended for research use only and is not for therapeutic or diagnostic use in humans. As a stable isotope, it is non-radioactive and poses minimal radiological risk. Its toxicological profile is expected to be similar to that of Mitotane, which can cause adrenal insufficiency and neurotoxicity at high doses.
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| References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Takeshita A, Igarashi-Migitaka J, Koibuchi N, Mitotane induces CYP3A4 expression via activation of the steroid and xenobiotic receptor. J Endocrinol. 2013 Feb 15;216(3):297-305. [3]. Doghman M, et al. Lack of long-lasting effects of mitotane adjuvant therapy in a mouse xenograft model of adrenocortical carcinoma. Mol Cell Endocrinol. 2013 Dec 5;381(1-2):66-9. [4]. Zatelli MC, et al. Therapeutic concentrations of mitotane (o,p'-DDD) inhibit thyrotroph cell viability and TSH expression and secretion in a mouse cell line model. Endocrinology. 2010 Jun;151(6):2453-61. [5]. Warde KM, et al. Mitotane Targets Lipid Droplets to Induce Lipolysis in Adrenocortical Carcinoma. Endocrinology. 2022 Sep 1;163(9):bqac102. |
| Additional Infomation |
Mitotane-13C6 is a high-purity (typically ≥98%) stable isotope-labeled compound with an isotopic enrichment of 99% ¹³C. It is used as an internal standard for the bioanalysis of Mitotane. This compound is an essential tool in drug development and clinical research for studying the pharmacokinetics and metabolism of Mitotane in the treatment of adrenocortical carcinoma.
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| Molecular Formula |
C813C6H10CL4
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|---|---|
| Molecular Weight |
326.00
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| Exact Mass |
325.97
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| CAS # |
1261396-21-7
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| Related CAS # |
Mitotane;53-19-0
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| PubChem CID |
49849664
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| Appearance |
White to off-white solid powder
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| LogP |
6.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
0
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
248
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C(=C1)C([13C]2=[13CH][13CH]=[13C]([13CH]=[13CH]2)Cl)C(Cl)Cl)Cl
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| InChi Key |
JWBOIMRXGHLCPP-CYRQOIGNSA-N
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| InChi Code |
InChI=1S/C14H10Cl4/c15-10-7-5-9(6-8-10)13(14(17)18)11-3-1-2-4-12(11)16/h1-8,13-14H/i5+1,6+1,7+1,8+1,9+1,10+1
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| Chemical Name |
1-chloro-2-[2,2-dichloro-1-(4-chloro(1,2,3,4,5,6-13C6)cyclohexa-1,3,5-trien-1-yl)ethyl]benzene
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0675 mL | 15.3374 mL | 30.6748 mL | |
| 5 mM | 0.6135 mL | 3.0675 mL | 6.1350 mL | |
| 10 mM | 0.3067 mL | 1.5337 mL | 3.0675 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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