An aromatase/CYP19A1 inhibitor
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Labeled Version(s)
25360Anastrozole-d12
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Anastrozole

Item No. 11987

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
α1,α1,α3,α3-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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 14 mg/mlDMSO: 13 mg/mlEthanol: 20 mg/mlEthanol: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    Cayman Chemical
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    Product Description

    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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Grimm, S.W., and Dyroff, M.C. Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab. Dispos. 25(5), 598-602 (1997).

    2. Plourde, P.V., Dyroff, M.C., and Dukes, M. Arimidex®: A potent and selective fourth-generation aromatase inhibitor. Breast 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 model. Anticancer Res. 28(5A), 2819-2823 (2008).