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Mitotane

Cat.No.S1732

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

Batch: Purity: 99.98%
99.98

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

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In vivo
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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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Chemical Information, Storage & Stability

Molecular Weight 320.04 Formula

C14H10Cl4

Storage (From the date of receipt)
CAS No. 53-19-0 Download SDF Storage of Stock Solutions

Synonyms NCI-C04933 SMILES C1=CC=C(C(=C1)C(C2=CC=C(C=C2)Cl)C(Cl)Cl)Cl

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Mechanism of Action

Targets/IC50/Ki
Sterol-O-Acyl Transferase 1
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. 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. 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.
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.
References
  • [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 2026-07-16)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03583710 RECRUITING
ENSAT Stage I Adrenal Cortex Carcinoma; ENSAT Stage II Adrenal Cortex Carcinoma; ENSAT Stage III Adrenal Cortex Carcinoma
M.D. Anderson Cancer Center
2018-08-20 PHASE3
NCT05913427 RECRUITING
Adrenocortical Carcinoma
Azienda Socio Sanitaria Territoriale degli Spedali Civili di Brescia
2022-06-08 PHASE2
NCT05036434 ACTIVE_NOT_RECRUITING
Adrenocortical Carcinoma
National Cancer Center, Korea
2021-11-15 PHASE2
NCT06831175 RECRUITING
Adrenal Cortical Carcinoma; Adrenal Cortical Cancer; Adrenal Cancer
West China Hospital
2025-03-15 PHASE2
NCT05634577 TERMINATED
Adrenocortical Carcinoma
M.D. Anderson Cancer Center
2023-03-23 PHASE2
NCT06279442 Not yet recruiting
Carcinoma Adrenal|Carcinoma Adrenocortical Recurrent
Latin American Cooperative Oncology Group
2024-06 --

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