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Mitotane
Synonyms: 米托坦, o,p'-DDD, NCI-C04933, Mitotan, 2,4′-DDD货号 T1199Cas号 53-19-0 一键复制产品信息纯度: 99.96%
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很棒Mitotane (NCI-C04933) 是 DDD 的同分异构体和 DDT 的衍生物，可作用于肾上腺皮质癌，有抗癌活性。
Mitotane
一键复制产品信息 很棒纯度: 99.96%
货号 T1199Cas号 53-19-0
别名 米托坦, o,p'-DDD, NCI-C04933, Mitotan, 2,4′-DDD
Mitotane (NCI-C04933) 是 DDD 的同分异构体和 DDT 的衍生物，可作用于肾上腺皮质癌，有抗癌活性。
其他形式的 “Mitotane”:
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mg | ¥ 139 | 现货 | |
| 25 mg | ¥ 208 | 现货 | |
| 50 mg | ¥ 293 | 现货 | |
| 100 mg | ¥ 423 | 现货 | |
| 500 mg | ¥ 693 | 现货 | |
| 1 g | ¥ 987 | 现货 |
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产品介绍
Mitotane AI Summary
Mitotane displays a high octanol-water partition coefficient with a log P value of 6.0, indicating significant lipophilicity and likely high membrane permeability. The compound exhibits a diverse range of bioactivities, presenting potency in numerous assays targeting various biological pathways. These include modulation of Lamin A splicing, JMJD2E inhibition, hypoxia response induction, mitochondrial division and fusion modulation, thyroid stimulating hormone receptor activation, TDP1 inhibition, mitochondrial channel activity inhibition, retinoid X receptor alpha signaling activation, inhibition of DNA re-replication, and inhibition of tumor cell line growth, indicating extensive pharmacological potential.
It also binds to and modulates several receptors and transporters, including adenosine A3, alpha-2A adrenergic, and various serotonin receptors and transporters, with moderate to high affinity (IC50/Ki values in the nM range). Despite this extensive bioactivity, Mitotane shows no induction of drug-induced liver injury, as indicated by a DILIps prediction score of 0.0 for various hepatic conditions, though some reports suggest moderate liver toxicity.
Further, it shows inhibitory activity against human BSEP and OATP1B1 and OATP1B3 transfected CHO cells. Its hepatobiliary transporter interactions suggest significant effects on bile acid and drug transport. Additionally, it has demonstrated antiviral activity against SARS-CoV-2, albeit with variable efficacy.
The compound is an inhibitor of human HDAC6, showing mild inhibition in enzymatic assays. It also induces CYP3A4, significantly reducing midazolam AUC by 94%, which highlights its role in drug metabolism. In receptor binding assays, it displays affinity towards multiple receptors (e.g., NR3C1, CNR1, AR, NR1I2, PGR), suggesting agonist or antagonist activity depending on the context.
Collectively, Mitotane stands out due to its wide spectrum of bioactivity, high lipophilicity, selective receptor interactions, antiviral potential, and specific enzymatic inhibition, with varied implications for pharmacological development and therapeutic application..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | 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. |
| 体外活性 | 在3小时内,60 mg/kg Mitotane分别显著降低大鼠的肾上腺线粒体、微粒体'P-450'和微粒体蛋白质的34％,55％和35％. |
| 体内活性 | 10-40 μM Mitotane抑制基底和cAMP诱导的皮质醇分泌,但不会引起细胞死亡。Mitotane对StAR和P450scc蛋白的基础表达具有抑制作用。40 μM Mitotane显著降低StAR,CYP11A1和CYP21的mRNA表达。H295R细胞中,Mitotane和吉西他滨联用显示出拮抗作用并干扰吉西他滨介导的细胞周期的S期抑制。Mitotane在小鼠TalphaT1细胞系中,抑制促甲状腺激素的表达和分泌,阻断促甲状腺激素对促甲状腺激素释放激素的应答,并且降低细胞活力,并诱导细胞凋亡。Mitotane在垂体促甲状腺激素分泌小鼠细胞中,不与甲状腺激素干预,而是直接减少了分泌活性和细胞活力。Mitotane诱发肾上腺皮质坏死,线粒体膜损伤,并且不可逆转的结合蛋白CYP。 |
| 别名 | 米托坦, o,p'-DDD, NCI-C04933, Mitotan, 2,4′-DDD |
| 分子量 | 320.04 |
| 分子式 | C14H10Cl4 |
| CAS No. | 53-19-0 |
| Smiles | ClC(Cl)C(c1ccc(Cl)cc1)c1ccccc1Cl |
| 密度 | 1.372 g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 250 mg/mL (781.15 mM), Sonication is recommended.  Ethanol: 60 mg/mL (187.48 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.25 mM), Sonication is recommended. 请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。 | ||||||||||||||||||||||||||||||||||||
计算器
体内实验配液计算器
请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：
比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL， 一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O， 那么您的工作液浓度为2 mg/mL。
母液配置方法：2 mg 药物溶于 100 μL DMSO （ 母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。
体内配方的制备方法： 取 100 μL DMSO 母液， 添加 400 μL PEG300 混匀澄清， 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
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