CAS 120511-73-1|Anastrozole

Introduction：Basic information about CAS 120511-73-1|Anastrozole, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Anastrozole BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Articles87
7. Synonyms

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	ChineseUSA	Flash Point	237.9±31.5 °C
Symbol	GHS07, GHS08	Signal Word	Danger

Names

Name	anastrozole
Synonym	More Synonyms

Anastrozole BiologicalActivity

Description	Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
Related Catalog	Signaling Pathways >>Others >>AromataseResearch Areas >>Cancer
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
InChIKey	YBBLVLTVTVSKRW-UHFFFAOYSA-N
SMILES	CC(C)(C#N)c1cc(Cn2cncn2)cc(C(C)(C)C#N)c1
Storage condition	Store at RT

Safety Information

Symbol	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

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

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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