产品
编 号:F381389
分子式:C14H10Cl4
分子量:320.04
产品类型
结构图
CAS No: 53-19-0
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生物活性:
Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions.
体内研究:
Mitotane (440 mg/kg;ip 或 po,每周 5 天,持续 7 周) 在 H295R 细胞接种后的早期时间点显著减少异种移植物的体积。Animal Model:NOD/SCID/γcnull mice (4-week-old; inoculated subcutaneously 6 × 106 H295R cells into the right flank)
Dosage:440 mg/kg
Administration:i.p. or p.o,; 5 days a week, for 7 weeks
Result:Significantly reduced the volume of xenografts at an early time point (day 13) after H295R cells inoculation.The effect of oral mitotane treatment became non-significant by day 20 after H295R cells inoculation, while the effect of i.p. mitotane lasted until day 34.
体外研究:
Mitotane (1 nM-100 μM;6 天) 显著降低 H295R 细胞增殖。Mitotane (10-100 μM;6 或 48 小时;TαT1 细胞) 以时间和剂量依赖的方式降低 TαT1 细胞活力;在60 μM至80 μM范围内显著且剂量依赖性地增加caspase 3/7活性。诱导TSH分泌和TSH β-亚基mRNA表达从40 μM 到 100 μM 的显著剂量依赖性降低。Mitotane (1-30 μM;24 小时;HepG2) 以剂量依赖性方式增加 CYP3A4 和 CYP2B6 基因的转录。Mitotane (20 和 40 μM;6 h) 显著减少了 HepaRG 中每个细胞的中性脂滴数量,也导致三酰甘油标记的脂滴显著减少;降低 PLIN1 和 PLIN3 的表达水平。