Mitotane

Catalog No.S1732 Batch:S173201

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Technical Data

Formula

C14H10Cl4
Molecular Weight 320.04 CAS No. 53-19-0
Solubility (25°C)* In vitro DMSO 64 mg/mL (199.97 mM)
Ethanol 64 mg/mL (199.97 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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]
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]

Protocol (from reference)

Cell Assay:

[5]
  • 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

Selleck's Mitotane has been cited by 20 publications

Albumin/Mitotane Interaction Affects Drug Activity in Adrenocortical Carcinoma Cells: Smoke and Mirrors on Mitotane Effect with Possible Implications for Patients' Management [ Int J Mol Sci, 2023, 24(23)16701] PubMed: 38069023
A 3D adrenocortical carcinoma tumor platform for preclinical modeling of drug response and matrix metalloproteinase activity [ Sci Rep, 2023, 13(1):15508] PubMed: 37726363
A 3D adrenocortical carcinoma tumor platform for preclinical modeling of drug response and matrix metalloproteinase activity [ Sci Rep, 2023, 13(1):15508] PubMed: 37726363
Single-cell multiomics analysis reveals regulatory programs in clear cell renal cell carcinoma [ Cell Discov, 2022, 8(1):68] PubMed: 35853872
Development of Human Pituitary Neuroendocrine Tumor Organoids to Facilitate Effective Targeted Treatments of Cushing's Disease [ Cells, 2022, 11(21)3344] PubMed: 36359740
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] PubMed: 35118583
Ribociclib Cytotoxicity Alone Or Combined With Progesterone And/Or Mitotane In In Vitro Adrenocortical Carcinoma Cells [ Endocrinology, 2021, bqab248] PubMed: 34875044
Estrogen-Like Effect of Mitotane Explained by Its Agonist Activity on Estrogen Receptor-α [ Biomedicines, 2021, 9(6)681] PubMed: 34208714
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] PubMed: 34383271

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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