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Anastrozole-d12 is intended for use as an internal standard for the quantification of anastrozole by GC- or LC-MS. Anastrozole is an aromatase/CYP19A1 inhibitor (IC50 = 15 nM for human placental aromatase/CYP19A1).1 It is selective for aromatase/CYP19A1 over the cytochrome P450 (CYP) isoforms CYP1A2, CYP2A6, CYP2C9, CYP2D6, and CYP3A (IC50s = 27-650 μM). Anastrozole (0.1 mg/kg) blocks ovulation in mature female rats and androstenedione-stimulated uterine development in pubertal female rats.2 It inhibits peripheral aromatase/CYP19A1 and reduces plasma estradiol concentrations in male pigtailed monkeys when administered at doses greater than 0.1 mg/kg. Anastrozole (0.5 mg/kg) reduces tumor incidence and the number of tumors by 40 and 57%, respectively, as well as increases latency to tumor appearance in a rat model of premenopausal mammary tumorigenesis.3 Formulations containing anastrozole have been used in the treatment of breast cancer.

1.Grimm, S.W., and Dyroff, M.C.Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromataseDrug Metabolism and Disposition25(5)598-602(1997) 2.Plourde, P.V., Dyroff, M.C., and Dukes, M.Arimidex®: A potent and selective fourth-generation aromatase inhibitorBreast Cancer Res. Treat.30(1)103-111(1994) 3.Kubatka, P., SadlonovÁ, V., Kajo, K., et al.Chemopreventive effects of anastrozole in a premenopausal breast cancer modelAnticancer Res.28(5A)2819-2823(2008).
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