Anastrozole

Modify Date: 2025-08-20 20:23:02

Anastrozole Structure
Anastrozole structure
 Common Name Anastrozole
CAS Number 120511-73-1 Molecular Weight 293.366
Density 1.1±0.1 g/cm3 Boiling Point 469.7±55.0 °C at 760 mmHg
Molecular Formula C17H19N5 Melting Point 81-82°C
MSDS Chinese USA Flash Point 237.9±31.5 °C
Symbol GHS07 GHS08
GHS07, GHS08		 Signal Word Danger

 Use of Anastrozole


Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.

 Names

Name anastrozole
Synonym More Synonyms

 Anastrozole Biological Activity

Description Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
Related Catalog
Target

IC50: 15 nM (human aromatase)[1]

In Vitro Anastrozole is a comparatively simple, achiral benzyltriazole derivative, that inhibits human placental aromatase with an IC50 of 15 nM. In the same assay it is 200 times as potent as aminoglutethimide (AG), twice as potent as 4-OHA and one third as potent as Fadrozole[1].
In Vivo Groups of eight immature (22-day-old) female rats are given androstenedione (AD) (30 mg/kg) in arachis oil s.c. daily for3 days with or without various doses of Anastrozole p.o. on day 4 the uteri are dissected, blotted and weighed. An oral dose of 0.1 mg/kg of Anastrozole given on day 2 or day 3 of the cycle completely blocked ovulation. At the same daily dosage (0.1 mg/kg), Anastrozole completely extinguished the uterotrophic activity of exogenous AD in immature rats. In male pigtailed monkeys, twice-daily oral treatment with 0.1 mg/kg and above of Anastrozole reduced circulating oestradiol concentrations by 50-60%[1].
Kinase Assay Aromatase inhibition is measured using human placental microsomes and the method of Thompson and Siiteri with Testosterone (0.5 μM) as substrate. 11-hydroxylase inhibition is determined by measuring the conversion of [1,2,6,7-3H]-ll-deoxy- cortisol to cortisol using freshly prepared mitochondria from guinea pig, dog and cow adrenal glands. Reaction products areextracted into chloroform and separated by thin layer chromatography[1].
Animal Admin Mice[1] Groups of at least eight adult female rats, housed in controlled lighting (on 06.00-20.00 h) and temperature (24±2°C) and undergoing 4-day oestrous cycles, are treated p.o. with a single dose of Anastrozole (0.01-0.1 mg/kg), Fadrozole (0.01-0.1 mg/kg) or AG (5-20 mg/kg) on day 2 at 16.00 h or day 3 at 12.00 h. The presence or absence of eggs in the oviducts on day 1 of the next cycle is then determined. Ovulation is considered blocked when no eggs are found.
References

[1]. Dukes M, et al. The preclinical pharmacology of "Arimidex" (anastrozole; ZD1033)--a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 469.7±55.0 °C at 760 mmHg
Melting Point 81-82°C
Molecular Formula C17H19N5
Molecular Weight 293.366
Flash Point 237.9±31.5 °C
Exact Mass 293.164032
PSA 78.29000
LogP 0.97
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.580
Storage condition Store at RT

 Safety Information

Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Danger
Hazard Statements H302-H360
Precautionary Statements P201-P280-P301 + P312 + P330-P308 + P313
Hazard Codes Xi
Risk Phrases R36/37/38
Safety Phrases 26-37/39
RIDADR 3249
RTECS CZ1465000
Packaging Group III
Hazard Class 6.1(b)
HS Code 2933990090

 Synthetic Route

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles87

More Articles
Changes in bone mineral density at 3 years in postmenopausal women receiving anastrozole and risedronate in the IBIS-II bone substudy: an international, double-blind, randomised, placebo-controlled trial.

Lancet Oncol. 15(13) , 1460-8, (2014)

Aromatase inhibitors prevent breast cancer in postmenopausal women at high risk of the disease but are associated with accelerated bone loss. We assessed effectiveness of oral risedronate for preventi...

NSAID use reduces breast cancer recurrence in overweight and obese women: role of prostaglandin-aromatase interactions.

Cancer Res. 74(16) , 4446-57, (2014)

Obesity is associated with a worse breast cancer prognosis and elevated levels of inflammation, including greater cyclooxygenase-2 (COX-2) expression and activity in adipose-infiltrating macrophages. ...

Impact of BMI on serum estradiol and bone turnover markers in postmenopausal women with hormone-sensitive early breast cancer treated with anastrozole.

J. Cancer Res. Clin. Oncol. 140(1) , 159-66, (2014)

Obesity increases the risk of all-cause and breast cancer mortality. As obese patients have higher levels of aromatase enzyme activity, conflicting results on the effect of body mass index (BMI) of a ...

 Synonyms

Anastrozole
ICI-D-1033
ZD-1033
2,2'-5-(1H-1,2,4-triazol-1-ylmethyl)benzene-1,3-diylbis(2-methylpropanenitrile)
Anastrol
MFCD00866298
1,3-Benzenediacetonitrile, α,α,α',α'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-
2,2'-[5-(1H-1,2,4-Triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropanenitrile)
ICI D 1033
1,3-benzenediacetonitrile
2,2'-[5-(1H-1,2,4-triazol-1-ylméthyl)benzène-1,3-diyl]bis(2-méthylpropanenitrile)
2,2'-[5-(1H-1,2,4-Triazol-1-ylmethyl)benzol-1,3-diyl]bis(2-methylpropanonitril)
ANASTRAZOLE
2,2'-(5-((1H-1,2,4-Triazol-1-yl)methyl)-1,3-phenylene)bis(2-methylpropanenitrile)
4-Triazol-1-ylmethyl)-1
Anastrolozole
Anatrozole
a,a,a',a'-Tetramethyl-5-(1H-,2,4-triazol-1-ylmethyl)-1,3-benzenediacetonitrile
Anastrozol
ARIMIDEX
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