Anastrozole

Catalog No.S1188

Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor.

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Anastrozole Chemical Structure

Anastrozole Chemical Structure
Molecular Weight: 293.37

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Product Information

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Product Description

Biological Activity

Description Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor.
Targets Aromatase [1]
IC50 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]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Dukes M, et al. J Steroid Biochem Mol Biol, 1996, 58(4), 439-445.

[2] Plourde PV, et al. Breast Cancer Res Treat, 1994, 30(1), 103-111.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02476786 Not yet recruiting Breast Cancer|Cancer of Breast|Breast Neoplasms|Cancer of the Breast Washington University School of Medicine|Genomic Health®,  ...more Washington University School of Medicine|Genomic Health®, Inc. August 2015 Phase 2
NCT02441946 Not yet recruiting Breast Cancer|Hormone Receptor Positive Tumor|Early-Stage Breast Carcinoma Eli Lilly and Company July 2015 Phase 2
NCT02206984 Not yet recruiting Breast Cancer University of Pittsburgh July 2015 --
NCT02440230 Recruiting Breast Cancer Shanghai Jiao Tong University School of Medicine May 2015 Phase 4
NCT02344472 Not yet recruiting Metastatic Breast Cancer Prof. W. Janni|University of Ulm April 2015 Phase 3

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Chemical Information

Download Anastrozole SDF
Molecular Weight (MW) 293.37
Formula

C17H19N5

CAS No. 120511-73-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms ZD-1033
Solubility (25°C) * In vitro DMSO 59 mg/mL (201.11 mM)
Ethanol 59 mg/mL (201.11 mM)
Water <1 mg/mL (<1 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.
Chemical Name  α1,​α1,​α3,​α3-​tetramethyl-​5-​(1H-​1,​2,​4-​triazol-​1-​ylmethyl)​- 1,​3-​benzenediacetonitril​e

Tech Support & FAQs

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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