Cat. No. Name Size Price Add Cart
KI0843Anastrozole10 mg$154
Anastrozole50 mg$432
Anastrozole100 mg$592

Chemical Characteristic

Product NameAnastrozole
SynonymsArimidex
CAS No.120511-73-1
Molecular Weight 293.37
FormulaC17H19N5
Chemical Structure
DocumentsCOA HNMR HPLC MS

Biological activities

Anastrozole is a potent and selective aromatase inhibitor with an IC50 value of 15 nM.[1] Anastrozole binds reversibly to the aromatase enzyme through competitively inhibiting the conversion of androgens to estrogens.[2] Anastrozole inhibits CYP1A2, CYP2C9, and CYP3A activities with Ki values of 8, 10, and 10 µM, respectively. However, anastrozole does not inhibit CYP2A6 and CYP2D6 activities at concentrations below 500 µM.[3] In vitro, anastrozole treatment (0.1-100 µM) leads to significant suppression of A549 and H23 lung tumor cells growth in a dose-dependent manner. Similarly, among ovariectomized nude mice with A549 lung tumor xenografts, administration of anastrozole (20 µg/mouse/day given by p.o. gavage) for 21 days elicites pronounced inhibition of lung tumor growth in vivo.[4] Anastrozole elicits maximal activity in vivo in rats (inhibition of ovulation and androstenedione-induced uterine hypertrophy) and monkeys (lowering of plasma oestradiol) at 0.1 mg/kg p.o.[1]

Protocols

In vivo: Anastrozole is dissolved in DMSO.[5]

References

[1] Dukes M, et al. The preclinical pharmacology of "Arimidex" (anastrozole; ZD1033)--a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996, 58(4): 439-445.
[2] Simpson ER, et al. Sources of estrogen and their importance. J Steroid Biochem Mol Biol. 2003, 86(3-5): 225-230. 閵嗏偓閵嗏偓
[3] Grimm SW, et al. Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos. 1997, 25(5): 598-602. 閵嗏偓閵嗏偓
[4] Weinberg OK, et al. Aromatase inhibitors in human lung cancer therapy. Cancer Res. 2005, 65(24): 11287-11291. 閵嗏偓閵嗏偓
[5] Moradpour F, et al. Anastrozole improved testosterone-induced impairment acquisition of spatial learning and memory in the hippocampal CA1 region in adult male rats. Behav Brain Res. 2006, 175(2): 223-232. 閵嗏偓閵嗏偓

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