Anastrozole

Catalog No.S1188 Batch:S118801

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Technical Data

Formula

C17H19N5

Molecular Weight 293.37 CAS No. 120511-73-1
Solubility (25°C)* In vitro DMSO 59 mg/mL (201.11 mM)
Ethanol 59 mg/mL (201.11 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids.
Targets
Aromatase [1]
(human placental microsomes)
15 nM
In vitro 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. [1]. 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. [2]
In vivo Anastrozole (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%. [2]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , Oncotarget, 2016, 7(34):54157-54173]

Data from [Data independently produced by , , Int J Oncol, 2015, 46(4):1481-90. ]

Selleck's Anastrozole has been cited by 29 publications

CDK4/6 inhibitors induce breast cancer senescence with enhanced anti-tumor immunogenic properties compared with DNA-damaging agents [ Mol Oncol, 2023, 10.1002/1878-0261.13541] PubMed: 37854019
SERPINA3-ANKRD11-HDAC3 pathway induced aromatase inhibitor resistance in breast cancer can be reversed by HDAC3 inhibition [ Commun Biol, 2023, 6(1):695] PubMed: 37414914
SERPINA3-ANKRD11-HDAC3 pathway induced aromatase inhibitor resistance in breast cancer can be reversed by HDAC3 inhibition [ Commun Biol, 2023, 6(1):695] PubMed: 37414914
SERPINA3-ANKRD11-HDAC3 pathway induced aromatase inhibitor resistance in breast cancer can be reversed by HDAC3 inhibition [ Commun Biol, 2023, 6(1):695] PubMed: 37414914
Dynamic O-GlcNAcylation coordinates ferritinophagy and mitophagy to activate ferroptosis [ Cell Discov, 2022, 8(1):40] PubMed: 35504898
CK2-induced cooperation of HHEX with the YAP-TEAD4 complex promotes colorectal tumorigenesis [ Nat Commun, 2022, 13(1):4995] PubMed: 36008411
Deficiency of WTAP in hepatocytes induces lipoatrophy and non-alcoholic steatohepatitis (NASH) [ Nat Commun, 2022, 13(1):4549] PubMed: 35927268
SARS-CoV-2 ORF10 antagonizes STING-dependent interferon activation and autophagy [ J Med Virol, 2022, 94(11):5174-5188] PubMed: 35765167
Pantothenate Kinase 1 Inhibits the Progression of Hepatocellular Carcinoma by Negatively Regulating Wnt/β-catenin Signaling [ Int J Biol Sci, 2022, 18(4):1539-1554] PubMed: 35280671
STING controls energy stress-induced autophagy and energy metabolism via STX17 [ J Cell Biol, 2022, 221(7)e202202060] PubMed: 35510944

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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