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Mitotane

Name: Mitotane
Brand: Selleck Chemicals
SKU: S1732
Availability: InStock
Rating: 5 (20 reviews)

Cat.No.S1732

Mitotane (NCI-C04933), is an antineoplastic medication used in the treatment of adrenocortical carcinoma.

Chemical Structure

Molecular Weight: 320.04

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.98%

99.98

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Chemical Information, Storage & Stability

Molecular Weight	320.04	Formula	C₁₄H₁₀Cl₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	53-19-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NCI-C04933			Smiles	C1=CC=C(C(=C1)C(C2=CC=C(C=C2)Cl)C(Cl)Cl)Cl

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (199.97 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 64 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.200mg/ml (10.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 64 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (2.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Sterol-O-Acyl Transferase 1 ^[5]
In vitro	Mitotane inhibits both TSH expression and secretion, blocks TSH response to TRH, and reduces cell viability, inducing apoptosis at concentrations in the therapeutic window in the mouse TalphaT1 cell line. This compound does not interfere with thyroid hormone laboratory tests but directly reduces both secretory activity and cell viability on pituitary TSH-secreting mouse cells. ^[1] It induces adrenal cortex necrosis, mitochondrial membrane impairment, and irreversible binding to CYP proteins. This chemical (10-40μM) inhibits basal and cAMP-induced cortisol secretion but does not cause cell death. It exhibits an inhibitory effect on the basal expression of StAR and P450scc protein. This agent (40 μM) significantly diminishes StAR, CYP11A1 and CYP21 mRNA expression. This compound (40μM) almost completely neutralizes this positive effect and returned 8-Br-cAMP-induced StAR, CYP11A1, CYP17 and CYP21 mRNA to control levels. ^[2] Its combination with gemcitabine shows antagonistic effects and interfered with the gemcitabine-mediated inhibition of the S phase of the cell cycle in H295R cells. ^[3]
In vivo	Mitotane (60 mg/kg) significantly decreases adrenal mitochondrial and microsomal "P-450" and microsomal protein content 34%, 55%, and 35% respectively in rats, within 3 hours. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/20392828/ [2] https://pubmed.ncbi.nlm.nih.gov/22546480/ [3] https://pubmed.ncbi.nlm.nih.gov/24018612/ [4] https://pubmed.ncbi.nlm.nih.gov/1257603/ [5] https://pubmed.ncbi.nlm.nih.gov/26305886/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06279442	Not yet recruiting	Carcinoma Adrenal\|Carcinoma Adrenocortical Recurrent	Latin American Cooperative Oncology Group	June 2024	--
NCT05344027	Completed	Adrenocortical Carcinoma	King''s College Hospital NHS Trust	April 11 2022	--
NCT02057237	Completed	Prostate Cancer	University Health Network Toronto	September 2013	Phase 1

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Handling Instructions

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