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Mitotane

Name: Mitotane
Brand: Selleck Chemicals
SKU: S1732
Rating: 5 (19 reviews)

Synonyms: NCI-C04933

Catalog No.S1732 Purity: 99.98%

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

Mitotane Chemical Structure

CAS: 53-19-0

Selleck's Mitotane has been cited by 19 publications

Purity & Quality Control

Batch: Purity: 99.98%

99.98

Mitotane Related Products

Biological Activity

Description

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

Targets

Sterol-O-Acyl Transferase 1 ^[5]

In vitro
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. Mitotane does not interfere with thyroid hormone laboratory tests but directly reduces both secretory activity and cell viability on pituitary TSH-secreting mouse cells. ^[1] Mitotane induces adrenal cortex necrosis, mitochondrial membrane impairment, and irreversible binding to CYP proteins. Mitotane (10-40μM) inhibits basal and cAMP-induced cortisol secretion but does not cause cell death. Mitotane exhibits an inhibitory effect on the basal expression of StAR and P450scc protein. Mitotane (40 μM) significantly diminishes StAR, CYP11A1 and CYP21 mRNA expression. Mitotane (40μM) almost completely neutralizes this positive effect and returned 8-Br-cAMP-induced StAR, CYP11A1, CYP17 and CYP21 mRNA to control levels. ^[2] Mitotane and gemcitabine combinations show antagonistic effects and interfered with the gemcitabine-mediated inhibition of the S phase of the cell cycle in H295R cells. ^[3]
Cell Research	Cell lines	NCI-H295 cells
	Concentrations	0-100 μM
	Incubation Time	24 or 72 h
	Method	NCI-H295 cells (10⁶/well) incubated with different concentrations of mitotane or diluent were collected and stained with fluorescein-isothiocyanate-labeled Annexin V for 15 minutes and for 2 minutes with propidium iodide at RT. After washing, fluorescence was measured by flow cytometry using a FACSCalibur instrument and data analyzed with Cell Quest Pro. Viability testing using WST1 reagent was performed according to manufacturer's protocol

In Vivo
In vivo	Mitotane (60 mg/kg) significantly decreases adrenal mitochondrial and microsomal "P-450" and microsomal protein contnet 34%, 55%, and 35% respectively in rats, within 3 hours. ^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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Chemical Information & Solubility

Molecular Weight	320.04	Formula	C₁₄H₁₀Cl₄
CAS No.	53-19-0	SDF	Download Mitotane SDF
Smiles	C1=CC=C(C(=C1)C(C2=CC=C(C=C2)Cl)C(Cl)Cl)Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 64 mg/mL ( (199.97 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 64 mg/mL

Water : Insoluble

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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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