Anastrozole

Catalog No.S1188

Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor.

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In DMSO USD 130 In stock
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Anastrozole Chemical Structure

Anastrozole Chemical Structure
Molecular Weight: 293.37

Validation & Quality Control

Quality Control & MSDS

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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

Protocol(Only for Reference)

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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 2014-11-22)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02269072 Not yet recruiting Hypertension Massachusetts General Hospital February 2015 --
NCT02278120 Not yet recruiting Advanced, Metastatic Breast Cancer Novartis Pharmaceuticals|Novartis November 2014 Phase 3
NCT02246621 Recruiting Breast Cancer Eli Lilly and Company November 2014 Phase 3
NCT02291913 Not yet recruiting Breast Cancer SCRI Development Innovations, LLC|Novartis November 2014 Phase 2
NCT02269670 Not yet recruiting Estrogen Receptor-positive Breast Cancer|HER2-negative Breast Cancer|Progesterone Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage III  ...more Estrogen Receptor-positive Breast Cancer|HER2-negative Breast Cancer|Progesterone Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Emory University|Novartis October 2014 Phase 2

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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 DMSO
Synonyms ZD-1033
Solubility (25°C) * In vitro DMSO 59 mg/mL (201.11 mM)
Water <1 mg/mL (<1 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.
Chemical Name  α1,​α1,​α3,​α3-​tetramethyl-​5-​(1H-​1,​2,​4-​triazol-​1-​ylmethyl)​- 1,​3-​benzenediacetonitril​e

Research Area

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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