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120511-73-1

120511-73-1 structure
120511-73-1 structure
  • Name: Anastrozole
  • Chemical Name: anastrozole
  • CAS Number: 120511-73-1
  • Molecular Formula: C17H19N5
  • Molecular Weight: 293.366
  • Catalog: API Antineoplastic agents Hormone antineoplastic agents
  • Create Date: 2018-06-10 16:20:11
  • Modify Date: 2024-01-01 20:44:47
  • Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
Name anastrozole
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
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.
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
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
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%

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title: CAS No. 120511-73-1 | Chemsrc address: https://m.chemsrc.com/en/baike/1026148.html

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