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Mitotane

Synonyms: NCI-C04933

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

Mitotane Chemical Structure

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

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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
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

Chemical lnformation & 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)

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
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