Catalog No.S1188 Synonyms: ZD-1033
Molecular Weight(MW): 293.37
Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor.
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Expression of ER, PR, Bcl-2 and HER receptors in MCF-7 and AI-resistant cell lines. Western blot analysis of protein expression in AI-resistant cell lines grown under standard conditions with their respective AI and MCF-7 cells grown with 1% FCS or grown with 10% NCS + 10−7 M testosterone for 21 weeks. β-actin was used as loading control.
Int J Oncol, 2015, 46(4):1481-90. . Anastrozole purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor.|
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. 
|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%. |
|In vitro||DMSO||59 mg/mL (201.11 mM)|
|Ethanol||59 mg/mL (201.11 mM)|
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02763566||Not yet recruiting||Breast Cancer||Eli Lilly and Company||October 2016||Phase 3|
|NCT02476786||Not yet recruiting||Breast Cancer|Cancer of Breast|Breast Neoplasms|Cancer of the Breast||Washington University School of Medicine|Genomic Health®, Inc.||October 2016||Phase 2|
|NCT02730923||Recruiting||Endometrial Carcinoma|Metastatic Carcinoma|Hormone Receptor Positive Tumor||Centre Leon Berard||April 2016||Phase 1|Phase 2|
|NCT02689921||Active, not recruiting||Breast Neoplasms||Midwestern Regional Medical Center||April 2016||Phase 2|
|NCT02753686||Recruiting||HR+ HER2- Postmenopausal Advanced Breast Cancer||Novartis Pharmaceuticals|Novartis||March 2016||--|
|NCT02648477||Recruiting||Estrogen Receptor Negative|Estrogen Receptor Positive|HER2/Neu Negative|Progesterone Receptor Negative|Progesterone Receptor Positive|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma||City of Hope Medical Center|National Cancer Institute (NCI)|Merck Sharp & Dohme Corp.||March 2016||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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