货号:A119463
同义名:
ZD1033; Anastrol
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | Aromatase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Exemestane |
+++
Aromatase (human), IC50: 30 nM Aromatase (rat), IC50: 40 nM |
97% | |||||||||||||||||
Letrozole | 95% | ||||||||||||||||||
Anastrozole |
+++
Aromatase, IC50: 15 nM |
97% | |||||||||||||||||
Obacunone |
+
Aromatase, IC50: 28.4 μM |
Nrf2 | 98% | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Aromatase is the only enzyme in vertebrates known to catalyse the biosynthesis of all oestrogens from androgens[3]. Anastrozole as an achiral triazole derivative is an aromatase inhibitor with IC50 value of 15 nM. Anastrozole has been shown to possess superior efficacy and tolerability over established endocrine agents in advanced breast cancer[4]. In vitro, anastrozole markedly inhibited breast cancer cell line MCF-7 cell proliferation at concentration ranging in 15 – 80 nM[5]. Administration of 1 μM anastrozole for 24h reduced mouse mammary carcinoma derived FM3A cell viability[6]. Treatment with 200 mg/mL and 300 mg/mL anastrozole significantly inhibited the growth of endometrioma cells and estradiol secretion[7]. In vivo, treatment with anastrozole on the dose of 200 μg/kg once a day established to be maximally effective in reducing tumor growth in the mouse intratumoral aromatase xenograph model[8]. Administration of 0.1 mg/kg anastrozole completely blocked ovulation and extinguished the uterotrophic activity of exogenous androstenedione in immature rats[9]. Treatment with anastrozole 1 or 10 mg reduced the percentage aromatization from 2.25% to 0.074% and 0.043% in post-menopausal women with a diagnosis of advanced or recurrent[10]. |
Dose | Mice: 25 mg/kg[3] (i.g.) Rat: 0.1 mg/kg - 20 mg/kg[4] (p.o.) |
Administration | i.g., p.o. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.41mL 0.68mL 0.34mL |
17.04mL 3.41mL 1.70mL |
34.09mL 6.82mL 3.41mL |
CAS号 | 120511-73-1 |
分子式 | C17H19N5 |
分子量 | 293.37 |
SMILES Code | CC(C)(C#N)C1=CC(C(C)(C#N)C)=CC(CN2C=NC=N2)=C1 |
MDL No. | MFCD00866298 |
别名 | ZD1033; Anastrol; HSDB 7462; CCRIS 9352; ICI-D 1033 |
运输 | 蓝冰 |
InChI Key | YBBLVLTVTVSKRW-UHFFFAOYSA-N |
Pubchem ID | 2187 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, room temperature |
溶解方案 |
DMSO: 105 mg/mL(357.91 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear PO 0.5% CMC-Na 40 mg/mL suspension |