product name
来曲唑, ≥98% (HPLC)
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to off-white
溶解性
DMSO: >50 mg/mL
创始人
Novartis
储存温度
2-8°C
SMILES字符串
N#CC(C=C1)=CC=C1C(N2C=NC=N2)C3=CC=C(C#N)C=C3
InChI
1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H
InChI key
HPJKCIUCZWXJDR-UHFFFAOYSA-N
基因信息
human ... CYP19A1(1588)
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应用
来曲唑已用于：
- 在类器官生长试验中测定其抑制力（48）
- 研究类固醇受体共激活因子1（SRC-1）介导的海马PSD-95内源性雌激素调节作用（49）
- 研究其对肿瘤诱导的痛觉过敏的作用 （50）
- 对大鼠进行激素干预（51）研究其对脂质运载蛋白-2（Lcn2）的作用（52）研究其对机械痛觉过敏和芳香化酶表达的作用（53）
生化/生理作用
来曲唑是一种佐剂，可用于治疗乳腺癌。
来曲唑是第三代非甾体芳香酶抑制剂。 它是芳香酶系统的竞争性抑制剂，因此可抑制雄激素向雌激素转化。来曲唑通过竞争性结合到该酶的细胞色素P450亚基的血红素上而抑制芳香酶，导致所有组织中雌激素的生物合成减少。
警示用语：
Warning
危险声明
危险分类
Repr. 2 - STOT RE 2
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Drugs for Pregnant and Lactating Women E-Book (2009)
Natalia Lagunas et al.
Frontiers in neuroanatomy, 16, 902218-902218 (2022-07-12)
Sex steroid hormones, such as androgens and estrogens, are known to exert organizational action at perinatal periods and activational effects during adulthood on the brain and peripheral tissues. These organizational effects are essential for the establishment of biological axes responsible
Bianca Posocco et al.
PloS one, 15(2), e0228822-e0228822 (2020-02-08)
A novel LC-MS/MS method was developed for the quantification of the new cyclin dependent kinase inhibitors (CDKIs) palbociclib and ribociclib and the aromatase inhibitor letrozole used in combinatory regimen. The proposed method is appropriate to be applied in clinical practice
Mothaffar F Rimawi et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 31(14), 1726-1731 (2013-04-10)
We previously reported the eradication of human epidermal growth factor receptor 2 (HER2)- amplified human xenografts in mice by inhibition of the HER2 pathway with lapatinib and trastuzumab to block all homo- and heterodimer signaling as well as by blockade
Rob Riemsma et al.
Current medical research and opinion, 28(8), 1263-1279 (2012-06-29)
Third-generation aromatase inhibitors (letrozole, anastrozole) have shown superior efficacy in early and advanced breast cancer compared with tamoxifen. For HR+, HER2+ MBC, combination of an AI with an anti-HER2 agent (lapatinib or trastuzumab) has shown clinical benefit. Six databases were
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