An aromatase/CYP19A1 inhibitor (IC50 = 15 nM for human placental aromatase/CYP19A1); selective for aromatase/CYP19A1 over CYP1A2

Anastrozole – 10 mg

Brand:
Cayman
CAS:
120511-73-1
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An aromatase/CYP19A1 inhibitor (IC50 = 15 nM for human placental aromatase/CYP19A1); selective for aromatase/CYP19A1 over CYP1A2, CYP2A6, CYP2C9, CYP2D6, and CYP3A (IC50s = 27-650 μM); blocks ovulation in mature female rats and androstenedione-stimulated uterine development in pubertal female rats at 0.1 mg/kg; inhibits peripheral aromatase/CYP19A1 and reduces plasma estradiol concentrations in male pigtailed monkeys at ≥0.1 mg/kg; reduces tumor incidence and the number of tumors well as increases latency to tumor appearance in a rat model of premenopausal mammary tumorigenesis at 0.5 mg/kg

Formal name: α1,α1,α3,α3-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-benzenediacetonitrile

Synonyms:  Anastrol|ICI-D 1033|ZD 1033

Molecular weight: 293.4

CAS: 120511-73-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Reproductive Biology

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