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    Anastrozole (ZD1033)
    Anastrozole (ZD1033)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1799
    CAS #: 120511-73-1Purity ≥98%

    Description: Anastrozole (formerly known as ZD-1033) is a potent, third-generation nonsteroidal and selective inhibitor of aromatase with an IC50 of 15 nM for inhibiting human placental aromatase. Anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast. Anastrozole has been reported to inhibit human placental aromatase with an IC50 value of 14.6 nM or 0.0043μg/ml.

    References: J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45; Breast Cancer Res Treat. 1994;30(1):103-11.

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    Molecular Weight (MW)293.37
    FormulaC17H19N5
    CAS No.120511-73-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 59 mg/mL (201.1 mM)
    Water: <1 mg/mL
    Ethanol: 59 mg/mL (201.1 mM)
    SMILESCC(C1=CC(CN2N=CN=C2)=CC(C(C)(C)C#N)=C1)(C)C#N
    Synonyms

    ZD-1033; ZD1033; ZD 1033; CCRIS 9352; HSDB 7462; ICI D1033; Anastrozole (ANAS); Trade name: Arimidex. 

    Chemical Name: 2,2'-(5-((1H-1,2,4-triazol-1-yl)methyl)-1,3-phenylene)bis(2-methylpropanenitrile)

    Exact Mass: 293.16405 


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    In Vitro

    In vitro activity: Anastrozole has high intrinsic potency in vitro and inhibits human placental aromatase with an IC50 of 15 nM. Anastrozole it is 200 times as potent as AG, twice as potent as 4-OHA and one third as potent as fadrozole. Anastrozole inhibits aromatase by binding competitively to the hem group of the CYP unit of the enzyme thereby reducing estrogen biosynthesis in the periphery and the breast. Anastrozole has little or no effect on other steroid hormones.


    Kinase Assay: Aromatase inhibition is measured using human placental microsomes and the method of Thompson and Siiteri with Testosterone (0.5 μM) as substrate. 11-hydroxylase inhibition is determined by measuring the conversion of [1,2,6,7-3H]-ll-deoxy- cortisol to cortisol using freshly prepared mitochondria from guinea pig, dog and cow adrenal glands. Reaction products are extracted into chloroform and separated by thin layer chromatography. 


    Cell Assay: Anastrozole is a comparatively simple, achiral benzyltriazole derivative, that inhibits human placental aromatase with an IC50 of 15 nM. In the same assay it is 200 times as potent as aminoglutethimide (AG), twice as potent as 4-OHA and one third as potent as Fadrozole.

    In VivoAnastrozole (0.1 mg/kg) given orally to mature rats on Day 2 or 3 of the estrous cycle, blocked ovulation in mature females; in pubertal rats, the same dose given for 3 days completely blocks androstenedione-stimulated uterine development. These effects may be attributes to inhibition of the normal preovulatory rise in ovarian follicular estrogen synthesis in mature females and to inhibition of metabolism of the exogenous androstenedione by the immature ovary in prepubertal females. Twice-daily administration of >9.1 mg/kg of Anastrozole given orally to male pigtailed monkeys inhibits peripheral aromatase, thereby reducing circulating estradiol concentrations by 50% to 60%. 
    Animal model Rats
    Formulation & Dosage 0.1 mg/kg; oral
    ReferencesJ Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45; Breast Cancer Res Treat. 1994;30(1):103-11.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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