| Name | Mitotane |
| Description | Mitotane (NCI-C04933) is a derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression. |
| In vitro | 10-40 μM Mitotane inhibited basal and cAMP-induced cortisol secretion but did not cause cell death.Mitotane inhibited basal expression of StAR and P450scc proteins.40 μM Mitotane significantly reduced mRNA expression of StAR, CYP11A1 and CYP21.In H295R cells, the mRNA expression of StAR, CYP11A1 and CYP21 was significantly reduced by Mitotane. In H295R cells, Mitotane in combination with gemcitabine showed antagonistic effects and interfered with gemcitabine-mediated S-phase inhibition of the cell cycle.Mitotane inhibited the expression and secretion of thyroid stimulating hormone (TSH), blocked TSH response to thyrotropin-releasing hormone (THRH), decreased cell viability, and induced apoptosis in the mouse TalphaT1 cell line.Mitotane inhibited the expression and secretion of pituitary thyrotropin secretory hormone (PTHS) and induced apoptosis in the pituitary thyrotropin secretory hormone (PSH) cells. Mitotane induced adrenocortical necrosis, mitochondrial membrane damage, and irreversible binding of the protein CYP in pituitary thyrotropin-secreting mouse cells, without interfering with thyroid hormones, and directly reduced secretory activity and cell viability. |
| In vivo | 10-40 μM Mitotane inhibited basal and cAMP-induced cortisol secretion but did not cause cell death.Mitotane inhibited basal expression of StAR and P450scc proteins.40 μM Mitotane significantly reduced mRNA expression of StAR, CYP11A1 and CYP21.In H295R cells, the mRNA expression of StAR, CYP11A1 and CYP21 was significantly reduced by Mitotane. In H295R cells, Mitotane in combination with gemcitabine showed antagonistic effects and interfered with gemcitabine-mediated S-phase inhibition of the cell cycle.Mitotane inhibited the expression and secretion of thyroid stimulating hormone (TSH), blocked TSH response to thyrotropin-releasing hormone (THRH), decreased cell viability, and induced apoptosis in the mouse TalphaT1 cell line.Mitotane inhibited the expression and secretion of pituitary thyrotropin secretory hormone (PTHS) and induced apoptosis in the pituitary thyrotropin secretory hormone (PSH) cells. Mitotane induced adrenocortical necrosis, mitochondrial membrane damage, and irreversible binding of the protein CYP in pituitary thyrotropin-secreting mouse cells, without interfering with thyroid hormones, and directly reduced secretory activity and cell viability. |
| Storage | Store under nitrogen | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 250 mg/mL (781.15 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.25 mM), Sonication is recommended.
Ethanol : 60 mg/mL (187.48 mM), Sonication is recommended.
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| Keywords | TαT1 | NCI-C-04933 | NCI-C 04933 | Mitotane | Inhibitor | inhibit | HepaRG | H295R | drug-drug interactions | corticotroph cells | cholesterol | Apoptosis | antineoplastic | Adrenodoxin | adrenocortical carcinoma |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | N,N-Dicyclohexylcarbodiimide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Tobacco Monomer Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
