Anastrozole

Anastrozole is an aromatase/CYP19A1 inhibitor (IC50 = 15 nM for human placental aromatase/CYP19A1). 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. 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. Formulations containing anastrozole have been used in the treatment of breast cancer.Formal Name: alpha1,alpha1,alpha3,alpha3-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-benzenediacetonitrile. CAS Number: 120511-73-1. Synonyms: Anastrol, ICI-D 1033, ZD 1033. Molecular Formula: C17H19N5. Formula Weight: 293.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 14 mg/ml, DMSO: 13 mg/ml, Ethanol: 20 mg/ml, Ethanol: PBS (pH 7.2) (1:9): 0.1 mg/ml. SMILES: CC(C)(C#N)C1=CC(CN2C=NC=N2)=CC(C(C)(C)C#N)=C1. InChi Code: InChI=1S/C17H19N5/c1-16(2,9-18)14-5-13(8-22-12-20-11-21-22)6-15(7-14)17(3,4)10-19/h5-7,11-12H,8H2,1-4H3. InChi Key: YBBLVLTVTVSKRW-UHFFFAOYSA-N.