2. Apoptosis
  3. Apoptosis
  4. Mitotane

Mitotane  (Synonyms: 2,4′-DDD; o,p'-DDD)

Cat. No.: HY-13690 Purity: 99.94%
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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.

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

Mitotane Chemical Structure

Mitotane Chemical Structure

CAS No. : 53-19-0

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Mitotane:

Mitotane Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Mitotane

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4].

IC50 & Target

Apoptosis[1]
In Vitro

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.

Mitotane Related Antibodies

Cell Proliferation Assay[1]

Cell Line: H295R cells
Concentration: 1 nM-100 μM
Incubation Time: 6 days
Result: Significantly reduced H295R cell proliferation with an IC50 of 22.8 μM.

Cell Viability Assay[2]

Cell Line: TαT1 cells
Concentration: 10, 40, 60, 80 and 100 μM
Incubation Time: 6 or 48 h
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.

RT-PCR[3]

Cell Line: HepaRG cells and human hepatocytes
Concentration: 0.1, 1, 10, 20, 30, or 40 μM
Incubation Time: 24 or 48 h
Result: Increased mRNA levels of CYP3A4 and CYP2B6.

Western Blot Analysis[4]

Cell Line: H295R
Concentration: 20, 40 and 50 μM
Incubation Time: 6 h
Result: Decreased the expression levels of PLIN1 and PLIN3.
In Vivo

Mitotane (440 mg/kg; i.p. or p.o,; 5 days a week, for 7 weeks) significantly reduces the volume of xenografts at an early time point after H295R cells inoculation[1].

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

Animal Model: NOD/SCID/γcnull mice (4-week-old; inoculated subcutaneously 6 × 106 H295R cells into the right flank)[1]
Dosage: 440 mg/kg
Administration: i.p. or p.o,; 5 days a week, for 7 weeks
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.
Clinical Trial
Molecular Weight

320.04

Formula

C14H10Cl4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C(C2=CC=CC=C2Cl)C(Cl)Cl)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1246 mL 15.6230 mL 31.2461 mL
5 mM 0.6249 mL 3.1246 mL 6.2492 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, 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.

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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 (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.
  • Protocol 2

    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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.94%

COA (251 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
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, 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
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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Mitotane 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.

Keywords:

Mitotane53-19-02,4′-DDD o,p'-DDDApoptosisantineoplasticadrenocortical carcinomacholesterolcorticotroph cellsdrug-drug interactionsH295RTαT1HepaRGInhibitorinhibitorinhibit

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