Anastrozole

目录号: GC10256纯度: >99.50%同义词: 阿那曲唑; ZD1033
An aromatase/CYP19A1 inhibitor

Anastrozole
Cas No.: 120511-73-1
规格价格库存数量操作
10mg¥336.00现货
1
50mg¥651.00现货
1
200mg¥1,722.00现货
1
500mg¥2,531.00现货
1
10mM (in 1mL DMSO)¥410.00现货
1

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产品描述 Description

Anastrozole (Arimidex,ZD1033) is a potent and selective inhibitor of aromatase with an IC50 value of 14.6 nM or 0.0043μg/ml [1].

Anastrozole has been reported to inhibit human placental aromatase with an IC50 value of 14.6 nM or 0.0043μg/ml. In addition, an oral concentration of 0.1mg/kg of anastrozole has been revealed to completely inhibit ovulation by given on day 2 or day 3 of the cycle. In immature rat, an oral concentration of 0.1mg/kg of anastrozole has also noted to completely extinguish the uterotrophic activity of exogenous AD. Apart from these, by guinea pig, dog and cow adrenal microsomes, anastrozole has been exhibited to suppress the conversion of 11-deoxycortisol to cortisol with mean IC50 values of 4.09μM,129μM and 11.9μM, respectively [1].

References:
[1] Dukes M1, Edwards PN, Large M, Smith IK, Boyle T. The preclinical pharmacology of "Arimidex" (anastrozole; ZD1033)--a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

MCF7, HepG2, and PC3 cell lines

Preparation method

The solubility of this compound in DMSO is >14.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

25-400 μg/mL, 24h

Applications

In MCF7, HepG2, and PC3 cell lines, Anastrozole at 400 μg/mL showed the most significant cytotoxic toward all cell lines. Anastrozole at 400 μg/mL exhibited inhibition rates of 58.4%, 41.7% and 26.6% on MCF7, HepG2, and PC3 cell lines, respectively. In MCF7 breast cancer cells, Anastrozole (200 μg/mL) increased nuclear intensity corresponding to apoptotic changes by 38% and increased cell membrane permeability by 17.3%. Anastrozole also significantly increased cytochrome c release.

Animal experiment [2]:

Animal models

adult female rats; mature male pigtailed monkeys (M. nernestrina)

Dosage form

Rats: 0.01-0.1 mg/kg, p.o., on day 2 at 16.00 h or day 3 at 12.00 hMonkeys: 0.003, 0.01, 0.03, 0.1, 0.3 and 1.0 mg/kg, p.o., twice daily (09.00 h and 16.00 h)

Application

In adult female rats, Anastrozole (0.1 mg/kg) given on day 2 or day 3 completely blocked ovulation. In male pigtailed monkeys, Anastrozole (0.1 mg/kg and above) reduced circulating oestradiol concentrations by 50-60%. The clearance half-life of anastrozole in the monkey was about 7h.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Hassan F1, El-Hiti GA, Abd-Allateef M, et al. Cytotoxicity anticancer activities of anastrozole against breast, liver hepatocellular, and prostate cancer cells. Saudi Med J. 2017 Apr;38(4):359-365.

[2] Dukes M1, Edwards PN, Large M, Smith IK, Boyle T. The preclinical pharmacology of "Arimidex" (anastrozole; ZD1033)--a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
120511-73-1
同义词
阿那曲唑; ZD1033
化学名
2-[3-(2-cyanopropan-2-yl)-5-(1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile
SMILES
CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N
分子式
C17H19N5
分子量
293.37 g/mol
溶解性
≥ 14.15mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol