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应用
阿那曲唑(芳香化酶抑制剂)已被用于:
- 在DNA片段分析中用作阳性对照
- 研究其与特级初榨橄榄油及其主要脂肪酸成分(omega-9 OA)对雌激素受体阳性乳腺癌细胞的作用
- 研究其对多形性胶质母细胞瘤体内模型存活率、细胞增殖和凋亡的影响
生化/生理作用
含有三唑官能团的阿那曲唑能够可逆地与芳香化酶的细胞色素P-450组分结合。这种结合会干扰芳香酶的催化特性,从而导致雌激素的合成受到抑制。
芳香化酶可将肾上腺雄激素转化为雌激素;这种酶活性是绝经后妇女雌激素的主要产生来源。 绝经后妇女雌激素受体阳性乳腺癌的一种治疗方法便是通过抑制芳香化酶。 阿那曲唑是一种非甾体苄基三唑衍生物,可通过竞争性抑制而对芳香化酶进行抑制,并用于治疗雌激素受体阳性的乳腺癌。 该化合物被认为是第三代II型芳香化酶抑制剂,因其与第一代、第二代抑制剂相比,针对其他甾体激素具有更强的选择性和更低的作用(如有)。
阿那曲唑是一种非甾体芳香酶抑制剂。
特点和优势
该化合物由AstraZeneca开发。要浏览其他药物开发化合物和批准的药物/候选药物列表,单击此处。
警示用语:
Danger
危险声明
危险分类
Acute Tox. 4 Oral - Repr. 1B
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Yanyan Hong et al.
Steroids, 76(8), 802-806 (2011-03-23)
Aromatase is the rate-limiting enzyme in estrogen biosynthesis. As a cytochrome P450, it utilizes electrons from NADPH-cytochrome P450 reductase (CPR) to produce estrogen from androgen. Estrogen is a key factor in the promotion of hormone-dependent breast cancer growth. Aromatase inhibitors
Novel acylated steroidal glycosides from Caralluma tuberculata induce caspase-dependent apoptosis in cancer cells
Waheed A, et al.
Journal of Ethnopharmacology, 137(3), 1189-1196 (2011)
P Dubsky et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 24(3), 640-647 (2012-10-05)
In early estrogen receptor (ER)-positive/HER2-negative breast cancer, the decision to administer chemotherapy is largely based on prognostic criteria. The combined molecular/clinical EndoPredict test (EPclin) has been validated to accurately assess prognosis in this population. In this study, the clinical relevance
Kutlwano R Xulu et al.
International journal of molecular sciences, 22(8) (2021-05-01)
Thromboembolic complications are a leading cause of morbidity and mortality in cancer patients. Cancer patients often present with an increased risk for thrombosis including hypercoagulation, so the application of antiplatelet strategies to oncology warrants further investigation. This study investigated the
P I Petkov et al.
SAR and QSAR in environmental research, 20(7-8), 657-678 (2009-12-22)
Cytochrome P450 aromatase is a key steroidogenic enzyme that converts androgens to estrogens in vertebrates. There is much interest in aromatase inhibitors (AIs) both because of their use as pharmaceuticals in the treatment of estrogen-sensitive breast cancers, and because a
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