Mitotane
Based on 5 publication(s) in Google Scholar
Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions.
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- Purity: 99.92%
- CAS No.: 53-19-0
- 화학식: C14H10Cl4
- 분자량:320.04
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Mitotane
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Customer Validation & Images
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RT-PCR
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WB
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
Biological Activity
Apoptosis[1]
Mitotane (1 nM-100 μM; 6 days) significantly reduces H295R cell proliferation[1].
Mitotane (10-100 μM; 6 or 48 h; TαT1 cells) reduces TαT1 cell viability in time- and dose-dependent manners; significantly and dose dependently increases caspase 3/7 activity from 60 μM to 80 μM; induced a significant and dose-dependent reduction in TSH secretion and TSH β-subunit mRNA expression from 40 μM to 100 μM[2].
Mitotane (1-30 μM; 24 h; HepG2) increases transcription of the CYP3A4 and CYP2B6 gene in a dose-dependent manner[3].
Mitotane (20 and 40 μM; 6 h) significantly reduces the number of neutral lipid droplets per cell in HepaRG, also induces a significant decrease in triacylglycerol-labeled lipid droplets; decreases the expression levels of PLIN1 and PLIN3[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H295R cells
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Concentration:1 nM-100 μM
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Incubation Time:6 days
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Result:Significantly reduced H295R cell proliferation with an IC50 of 22.8 μM.
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Cell Line:TαT1 cells
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Concentration:10, 40, 60, 80 and 100 μM
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Incubation Time:6 or 48 h
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Result:Did not modify cell viability at 10-80 μM, while significantly (P < 0.01) reduced cell viability (-56%) at 100 μM, after 6 h incubation.
Did not modify cell viability at 10-60 μM, whereas cell viability was significantly reduced at 60 μM (-31%; P < 0.05), 80 μM (-53%; P < 0.01), and 100 μM (-75.5%; P < 0.01), after 48 h incubation.
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Cell Line:HepaRG cells and human hepatocytes
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Concentration:0.1, 1, 10, 20, 30, or 40 μM
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Incubation Time:24 or 48 h
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Result:Increased mRNA levels of CYP3A4 and CYP2B6.
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Cell Line:H295R
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Concentration:20, 40 and 50 μM
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Incubation Time:6 h
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Result:Decreased the expression levels of PLIN1 and PLIN3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID/γcnull mice (4-week-old; inoculated subcutaneously 6 × 106 H295R cells into the right flank)[1]
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Dosage:440 mg/kg
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Administration:i.p. or p.o,; 5 days a week, for 7 weeks
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Result:Significantly reduced the volume of xenografts at an early time point (day 13) after H295R cells inoculation.
The effect of oral mitotane treatment became non-significant by day 20 after H295R cells inoculation, while the effect of i.p. mitotane lasted until day 34.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 53-19-0
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Appearance Solid
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분자량 320.04
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화학식 C14H10Cl4
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Color White to off-white
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SMILES
ClC1=CC=C(C(C2=CC=CC=C2Cl)C(Cl)Cl)C=C1
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Synonyms
2,4′-DDD; o,p'-DDD
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Biomed Pharmacother
Targeting ER stress in adrenocortical carcinoma: Celastrol as a novel therapeutic candidate. [Abstract]2026 Feb 25:197:119156. PMID: 41747473 -
Biomed Pharmacother
Mitotane activates ATF4/ATF3 axis triggering endoplasmic reticulum stress in adrenocortical carcinoma cells. [Abstract]2025 Mar:184:117917. PMID: 39965324
Mitotane purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Mar:184:117917. [Abstract]
ddPCR quantification of ATF4 gene expression regulation induced by Mitotane (0, 5, 10, 15, 20 μM) treatment.
Mitotane purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Mar:184:117917. [Abstract]
Western blot quantification of ATF4 protein expression regulation induced by Mitotane (0, 10, 20 μM) treatment.
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J Transl Med
CDK1 serves as a therapeutic target of adrenocortical carcinoma via regulating epithelial-mesenchymal transition, G2/M phase transition, and PANoptosis. [Abstract]2022 Oct 2;20(1):444. PMID: 36184616
Mitotane purchased from MedChemExpress. Usage Cited in: J Transl Med. 2022 Oct 2;20(1):444. [Abstract]
Images of xenograft tumors of each group. Animal experiments were grouped as follows: vehicle, Mitotane (Mtn) (40 mg/kg), CurE (10 mg/kg), CurE (20 mg/kg) and co-administration of Mtn (40 mg/kg) and CurE (10 mg/kg).
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Front Endocrinol (Lausanne)
Pharmacogenomic analysis in adrenocortical carcinoma reveals genetic features associated with mitotane sensitivity and potential therapeutics. [Abstract]2024 May 8:15:1365321. PMID: 38779454
Mitotane purchased from MedChemExpress. Usage Cited in: Front Endocrinol (Lausanne). 2024 May 8:15:1365321. [Abstract]
Cell viability inhibition at 50 µM Mitotane for each individual primary cultures and determination of responders (red) and non-responders (grey). Mitotane-sensitive ACC cell line H295R was used as the positive control.
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618
용액&용해도
DMSO : ≥ 100 mg/mL (312.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.81 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.81 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (283 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
References
[1]. 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. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
[4]. Warde KM, et al. Mitotane Targets Lipid Droplets to Induce Lipolysis in Adrenocortical Carcinoma. Endocrinology. 2022 Sep 1;163(9):bqac102. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.1246 mL | 15.6230 mL | 31.2461 mL | 78.1152 mL |
| 5 mM | 0.6249 mL | 3.1246 mL | 6.2492 mL | 15.6230 mL | |
| 10 mM | 0.3125 mL | 1.5623 mL | 3.1246 mL | 7.8115 mL | |
| 15 mM | 0.2083 mL | 1.0415 mL | 2.0831 mL | 5.2077 mL | |
| 20 mM | 0.1562 mL | 0.7812 mL | 1.5623 mL | 3.9058 mL | |
| 25 mM | 0.1250 mL | 0.6249 mL | 1.2498 mL | 3.1246 mL | |
| 30 mM | 0.1042 mL | 0.5208 mL | 1.0415 mL | 2.6038 mL | |
| 40 mM | 0.0781 mL | 0.3906 mL | 0.7812 mL | 1.9529 mL | |
| 50 mM | 0.0625 mL | 0.3125 mL | 0.6249 mL | 1.5623 mL | |
| 60 mM | 0.0521 mL | 0.2604 mL | 0.5208 mL | 1.3019 mL | |
| 80 mM | 0.0391 mL | 0.1953 mL | 0.3906 mL | 0.9764 mL | |
| 100 mM | 0.0312 mL | 0.1562 mL | 0.3125 mL | 0.7812 mL |
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