Anastrozole - CAS 120511-73-1
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Anastrozole
Catalog Number:
B0084-311426
Synonyms:
ZD-1033; Arimidex; Anastrazole; Anastrozol; ZD1033
CAS Number:
120511-73-1
Description:
Anastrozole is an aromatase inhibitor that acts via 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. It is commonly used as therapy of estrogen receptor positive breast cancer.
Molecular Weight:
293.37
Molecular Formula:
C17H19N5
COA:
Inquire
MSDS:
Inquire
Canonical SMILES:
CC(C)(C#N)C1=CC(=CC(=C1)CN2C=NC=N2)C(C)(C)C#N
InChI:
InChI=1S/C17H19N5/c1-16(2,9-18)14-5-13(8-22-12-20-11-21-22)6-15(7-14)17(3,4)10-19/h5-7,11-12H,8H2,1-4H3
InChIKey:
YBBLVLTVTVSKRW-UHFFFAOYSA-N
Targets:
Cytochrome P450
Catalog Number Size Price Stock Quantity
B0084-311426 500 mg $298 In stock
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Chemical Structure
CAS 120511-73-1 Anastrozole

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Reference Reading


1.Phase II Randomized Preoperative Window-of-Opportunity Study of the PI3K Inhibitor Pictilisib Plus Anastrozole Compared With Anastrozole Alone in Patients With Estrogen Receptor-Positive Breast Cancer.
Schmid P1, Pinder SE2, Wheatley D2, Macaskill J2, Zammit C2, Hu J2, Price R2, Bundred N2, Hadad S2, Shia A2, Sarker SJ2, Lim L2, Gazinska P2, Woodman N2, Korbie D2, Trau M2, Mainwaring P2, Gendreau S2, Lackner MR2, Derynck M2, Wilson TR2, Butler H2, Earl J Clin Oncol. 2016 Mar 14. pii: JCO639179. [Epub ahead of print]
PURPOSE: Preclinical data support a key role for the PI3K pathway in estrogen receptor-positive breast cancer and suggest that combining PI3K inhibitors with endocrine therapy may overcome resistance. This preoperative window study assessed whether adding the PI3K inhibitor pictilisib (GDC-0941) can increase the antitumor effects of anastrozole in primary breast cancer and aimed to identify the most appropriate patient population for combination therapy.
2.Effect of MRP2 and MRP3 Polymorphisms on Anastrozole Glucuronidation and MRP2 and MRP3 Gene Expression in Normal Liver Samples.
Edavana VK1, Penney RB2, Yao-Borengasser A1, Starlard-Davenport A1, Dhakal IB1, Kadlubar S1. Int J Cancer Res Mol Mech. 2015 Oct;1(3). doi: 10.16966/2381-3318.112. Epub 2015 Sep 22.
Anastrozole is an aromatase inhibitor (AI) used as adjuvant therapy for breast cancer. Anastrozole is subject to direct glucuronidation catalyzed by UDP-glucuronosyltransferase1A4 (UGT1A4). Interindividual variability in anastrozole glucuronidation may be affected by UGT1A4 SNPs. Interplay between drug metabolizing genes such as UGT1A4 and transporter genes may also be affected by genetic variability. Thus, we hypothesize that genetic variability in MRPs could influence anastrozole glucuronidation. The correlation between UGT1A4 and MRP2 or MRP3 transporter gene expressions and the correlation between MRP2 or MRP3 mRNA and anastrozole glucuronidation were analyzed in normal human liver samples. MRP2 and MRP3 mRNA levels were significantly correlated with UGT1A4 mRNA, with anastrozole glucuronidation and with each other (p<0.05). The data also demonstrated that MRP2 SNPs are positively correlated with MRP2 mRNA expression, while there was no association between MRP3 SNPs from this study and MRP3 expression.
3.Pictilisib Plus Anastrozole Reduces Proliferation in ER+ Breast Cancer.
Cancer Discov. 2016 Mar 24. [Epub ahead of print]
The PI3K inhibitor pictilisib plus anastrozole suppresses luminal B breast cancer proliferation.
4.The association between pre-treatment occupational skill level and mood and symptom burden in early-stage, postmenopausal breast cancer survivors during the first year of anastrozole therapy.
Nugent BD1, Sereika SM1, Rosenzweig M1, McCue M2, Merriman JD1, Bender CM3. Support Care Cancer. 2016 Mar 17. [Epub ahead of print]
PURPOSE: Previous research has explored occupational activity of breast cancer survivors but has not examined the influence of occupational level on symptoms prospectively. The purpose of this study was to examine the relationship between occupational classification and changes in mood and symptom burden for postmenopausal breast cancer survivors during the first year of anastrozole therapy.