Shelf life (days): 1460.0
Formulation: A solid
Formal Name: a,a,a',a'-tetra(methyl-d3)-5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-benzenediacetonitrile
Purity: ≥99% deuterated forms (d1-d12)
Formula Markup: C17H7D12N5
Formula Weight: 305.43918
CAS Number: 120512-32-5
Notes: Anastrozole-d12 is intended for use as an internal standard for the quantification of anastrozole (Item No. 11987) by GC- or LC-MS. Anastrozole is an aromatase/CYP19A1 inhibitor (IC50 = 15 nM for human placental aromatase/CYP19A1).{21405} 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.{43283} 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.{43284} Formulations containing anastrozole have been used in the treatment of breast cancer.
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