Mitotane

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Chemical Structure| 53-19-0 同义名 : 2,4′-DDD; o,p'-DDD; Mytotan; Khloditan; Chlodithane; WR13045; CB313; NSC 38721; 1,1-Dichlorodiphenildichloroethane
CAS号 : 53-19-0
货号 : A817688
分子式 : C14H10Cl4
纯度 : 99%
分子量 : 320.04
MDL号 : MFCD00000850
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(328.08 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Mitotane is a steroidogenesis inhibitor and cytostatic antineoplastic medication which is used in the treatment of adrenocortical carcinoma and Cushing's syndrome. In the AtT20/D16v-F2 cell line and in primary cultures, mitotane reduces cell viability by inducing caspase-mediated apoptosis and reduces ACTH secretion. In the AtT20/D16v-F2 cell line, mitotane reduces Pomc expression and blocks the stimulatory effects of corticotropin-releasing hormone on cell viability, ACTH secretion, and Pomc expression[3]. Among the oxysterols detected in mitotane-treated cells, 27OHC was markedly produced, as well as lanosterol and lathosterol cholesterol precursors. In this cell model, mitotane was confirmed to affect mitochondrial transmembrane potential and induce apoptosis. Such cytotoxic effects were perfectly matched by H295R cell treatment with a single identical micromolar amount of 27OHC[4]. Treatment with mitotane (50 µM for 24 h) decreased the viability of FTC‑133, BCPAP, SW1736, C643 and TT cells by 12, 59, 54, 31 and 66%, respectively. Mitotane elicited pleiotropic effects on TC (thyroid cancer) cells, including induction of ER (endoplasmic reticulum) stress, inhibition of mitochondrial membrane potential and induction of apoptosis[5]. In addition, low-dose mitotane can trigger neurological and endocrinological complications in a pediatric patient; the drug dose should be individualized with frequent monitoring of the therapeutic level[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00453674 - Recruiting December 2025 Germany ... 展开 >> University of Wuerzburg Recruiting Wuerzburg, Germany, 97080 Contact: Martin Fassnacht, MD       fassnacht_m@medizin.uni-wuerzburg.de 收起 <<
NCT02788201 Urothelial Carcinoma ... 展开 >> Bladder Cancer Urinary Bladder Neoplasms 收起 << Phase 2 Recruiting July 1, 2020 United States, Maryland ... 展开 >> National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact National Cancer Institute Referral Office    888-624-1937 收起 <<
NCT03257891 Adrenocortical Carcinoma Phase 2 Recruiting January 24, 2022 Italy ... 展开 >> Azienda Ospedaliera Spedali Civili di Brescia Recruiting Brescia, Italy, 25123 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.62mL

3.12mL

1.56mL

31.25mL

6.25mL

3.12mL
参考文献

[1]Lin CW, Chang YH, et al. Mitotane exhibits dual effects on steroidogenic enzymes gene transcription under basal and cAMP-stimulating microenvironments in NCI-H295 cells. Toxicology. 2012 Aug 16;298(1-3):14-23.

[2]Zatelli MC, Gentilin E, et al. Therapeutic concentrations of mitotane (o,p'-DDD) inhibit thyrotroph cell viability and TSH expression and secretion in a mouse cell line model. Endocrinology. 2010 Jun;151(6):2453-61.

[3]Gentilin E, Tagliati F, Terzolo M, Zoli M, Lapparelli M, Minoia M, Ambrosio MR, Degli Uberti EC, Zatelli MC. Mitotane reduces human and mouse ACTH-secreting pituitary cell viability and function. J Endocrinol. 2013 Jul 29;218(3):275-85

[4]Germano A, Rossin D, Leoni V, Iaia N, Saba L, Basile V, Puglisi S, Caccia C, Poli G, Biasi F, Terzolo M. Involvement of 27-Hydroxycholesterol in Mitotane Action on Adrenocortical Carcinoma. Cells. 2020 Apr 4;9(4):885

[5]Bikas A, Jensen K, Patel A, Costello J, Kaltsas G, Hoperia V, Wartofsky L, Burman K, Vasko V. Mitotane induces mitochondrial membrane depolarization and apoptosis in thyroid cancer cells. Int J Oncol. 2019 Jul;55(1):7-20

[6]Heo YJ, Yoo JH, Choe YS, Park SH, Lee SB, Kim HA, Choi JY, Lee YA, Lim BC, Chueh HW. Low dose mitotane-induced neurological and endocrinological complication in a 5-year-old girl with adrenocortical carcinoma. Ann Pediatr Endocrinol Metab. 2021 Oct 18