Anastrozole

产品说明书

Print
Chemical Structure| 120511-73-1 同义名 : ZD1033; Anastrol; HSDB 7462; CCRIS 9352; ICI-D 1033
CAS号 : 120511-73-1
货号 : A119463
分子式 : C17H19N5
纯度 : 97%
分子量 : 293.37
MDL号 : MFCD00866298
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
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

生物活性
靶点

  • Aromatase

    Aromatase, IC50:15 nM
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].
实验方案
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
参考文献

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

[2]Plourde PV, Dyroff M, et al. Arimidex: a potent and selective fourth-generation aromatase inhibitor. Breast Cancer Res Treat. 1994;30(1):103-11.

[3]Ghosh D, Griswold J, Erman M, Pangborn W. Structural basis for androgen specificity and oestrogen synthesis in human aromatase. Nature. 2009 Jan 8;457(7226):219-23.

[4]Grimm SW, Dyroff MC. Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos. 1997 May;25(5):598-602.

[5]Alyafee YA, Alaamery M, Bawazeer S, Almutairi MS, Alghamdi B, Alomran N, Sheereen A, Daghestani M, Massadeh S. Preparation of anastrozole loaded PEG-PLA nanoparticles: evaluation of apoptotic response of breast cancer cell lines. Int J Nanomedicine. 2017 Dec 28;13:199-208.

[6]Topcul M, Cetin I, Ozlem Kolusayin Ozar M. The effects of anastrozole on the proliferation of FM3A cells. J BUON. 2013 Oct-Dec;18(4):874-8.

[7]Badawy SZ, Brown S, Kaufman L, Wojtowycz MA. Aromatase inhibitor (anastrozole) affects growth of endometrioma cells in culture. Eur J Obstet Gynecol Reprod Biol. 2015 May;188:45-50.

[8]Mast N, Lin JB, Pikuleva IA. Marketed Drugs Can Inhibit Cytochrome P450 27A1, a Potential New Target for Breast Cancer Adjuvant Therapy. Mol Pharmacol. 2015 Sep;88(3):428-36.

[9]Dukes M, 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.

[10]Geisler J, King N, Dowsett M, Ottestad L, Lundgren S, Walton P, Kormeset PO, Lønning PE. Influence of anastrozole (Arimidex), a selective, non-steroidal aromatase inhibitor, on in vivo aromatisation and plasma oestrogen levels in postmenopausal women with breast cancer. Br J Cancer. 1996 Oct;74(8):1286-91.