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Mitotane/米托坦 {[allProObj[0].p_purity_real_show]}

货号:A817688 同义名: 2,4′-DDD; o,p'-DDD

Mitotane是一种甾体生成抑制剂,用于治疗肾上腺皮质癌和库欣综合症。它通过诱导细胞内胆固醇积累引发脂毒性,抑制肾上腺皮质功能,并激活 CYP3A4 基因表达,表现出显著的抗肿瘤作用。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Mitotane/米托坦 化学结构 CAS号:53-19-0
Mitotane/米托坦 化学结构
CAS号:53-19-0
Mitotane/米托坦 3D分子结构
CAS号:53-19-0
Mitotane/米托坦 化学结构 CAS号:53-19-0
Mitotane/米托坦 3D分子结构 CAS号:53-19-0
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Mitotane/米托坦 纯度/质量文件 产品仅供科研

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Mitotane/米托坦 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].

Mitotane/米托坦 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 <<

Mitotane/米托坦 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

Mitotane/米托坦 实验方案

计算器
存储液制备 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

Mitotane/米托坦 技术信息

CAS号53-19-0
分子式C14H10Cl4
分子量 320.04
SMILES Code ClC1=CC=C(C(C2=CC=CC=C2Cl)C(Cl)Cl)C=C1
MDL No. MFCD00000850
别名 2,4′-DDD; o,p'-DDD; Mytotan; Khloditan; Chlodithane; WR13045; CB313; NSC 38721; 1,1-Dichlorodiphenildichloroethane
运输蓝冰
InChI Key JWBOIMRXGHLCPP-UHFFFAOYSA-N
Pubchem ID 4211
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, room temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
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