Anastrozole
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
阿那曲唑(Anastrozole)(Arimidex,ZD1033)是有效的选择性芳香酶抑制剂,IC50值为14.6 nM或0.0043 μg/ml[1].
阿那曲唑(Anastrozole)可抑制人胎盘芳香酶,IC50值为14.6 nM或0.0043 μg/ml.除此之外,在周期的第2或第3天时,以0.1 mg/kg浓度口服给药,anastrozole完全抑制排卵.在幼鼠中,以0.1 mg/kg浓度口服给药,anastrozole也可完全消除外源性AD的子宫营养活性.除此之外,通过对豚鼠\狗和牛肾上腺微粒体测试,anastrozole抑制11-脱氧可的松向皮质醇的转化,平均IC50值分别为4.09 μM\129 μM和11.9 μM[1].
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 293.37 |
Cas No. | 120511-73-1 |
Formula | C17H19N5 |
Solubility | insoluble in H2O; ≥14.15 mg/mL in DMSO; ≥8.62 mg/mL in EtOH |
Chemical Name | 2-[3-(2-cyanopropan-2-yl)-5-(1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile |
SDF | Download SDF |
Canonical SMILES | CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
MCF7,HepG2和PC3细胞系 |
溶解方法 |
该化合物在DMSO中的溶解度>14.2mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
25-400 μg/mL, 24h |
应用 |
在MCF7,HepG2和PC3细胞系中,400μg/ mL的Anastrozole对所有细胞系显示出最显著的细胞毒性。400μg/ mL的Anastrozole对MCF7,HepG2和PC3细胞系的抑制率分别为58.4%,41.7%和26.6%。在MCF7乳腺癌细胞中,Anastrozole(200μg/ mL)将对应于凋亡变化的细胞核强度提高38%,细胞膜通透性增加17.3%。Anastrozole也显著增加细胞色素c的释放。 |
动物实验[2]: | |
动物模型 |
成年雌性大鼠,成熟雄性豚尾猴(M.nernestrina) |
剂量 |
大鼠: 0.01-0.1 mg/kg,口服,在第2天16.00小时或第3天12.00小时猴子:0.003,0.01,0.03,0.1,0.3和1.0mg / kg,口服,每天两次(09.00h和16.00h) |
应用 |
在成年雌性大鼠中,在第2天或第3天给予Anastrozole(0.1mg / kg)完全阻止了排卵。在雄性豚尾猴中,Anastrozole(0.1mg / kg及以上)将循环雌二醇浓度降低了50-60%。Anastrozole在猴子中的清除半衰期约为7h。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。 |
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. |
质量控制和MSDS
- 批次: