Mitotane

製品コードS1732 バッチS173202

印刷

化学情報

Chemical Structure Synonyms NCI-C04933 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H10Cl4
分子量 320.04 CAS No. 53-19-0
Solubility (25°C)* 体外 DMSO 64 mg/mL (199.97 mM)
Ethanol 64 mg/mL warmed with 50ºC water bath (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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Mitotane (NCI-C04933), is an antineoplastic medication used in the treatment of adrenocortical carcinoma.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 NCI-H295 cells
濃度 0-100 μM
反応時間 24 or 72 h
実験の流れ

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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
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
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] PubMed: 34731453

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。