Catalog No.S1732 Synonyms: NCI-C04933
Molecular Weight(MW): 320.04
Mitotane, is an antineoplastic medication used in the treatment of adrenocortical carcinoma.
Purity & Quality Control
|Description||Mitotane, is an antineoplastic medication used in the treatment of adrenocortical carcinoma.|
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.  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.  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. 
|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. |
-  Zatelli MC, et al. Endocrinology,?010, 151(6), 2453-2561.
-  Lin CW, et al. Toxicology,?012, 298(1-3), 14-23.
-  Germano A, et al. Mol Cell Endocrinol. 2014, 382(1):1-7.
|In vitro||DMSO||64 mg/mL (199.97 mM)|
|Ethanol||64 mg/mL warmed (199.97 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02057237||Completed||Prostate Cancer||University Health Network, Toronto||September 2013||Phase 1|
|NCT00778817||Terminated||Recurrent Adrenocortical Carcinoma|Stage III Adrenocortical Carcinoma|Stage IV Adrenocortical Carcinoma||National Cancer Institute (NCI)||December 2008||Phase 2|
|NCT00777244||Unknown status||Adrenocortical Carcinoma||University of Turin, Italy||April 2008||Phase 3|
|NCT00304070||Active, not recruiting||Stage I Adrenocortical Carcinoma|Stage II Adrenocortical Carcinoma|Stage III Adrenocortical Carcinoma|Stage IV Adrenocortical Carcinoma||Childrens Oncology Group|National Cancer Institute (NCI)||September 2006||Phase 3|
|NCT00094497||Completed||Carcinoma, Adrenal Cortical||Collaborative Group for Adrenocortical Carcinoma Treatment|German Federal Ministry of Education and Research|National Cancer Institute (NCI)||June 2004||Phase 3|
|NCT00001339||Completed||Adrenal Cortical Carcinoma||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||August 1993||Phase 2|
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