Anastrozole

SKU: orb1310655

Description

Anastrozole

Research Area

Metabolism Research

Key Properties

• CAS Number: 120511-73-1
• MW: 293.37
• Purity: 99.96%
• Formula: C₁₇H₁₉N₅
• SMILES: C(C#N)(C)(C)C1=CC(C(C#N)(C)C)=CC(CN2C=NC=N2)=C1
• Target: Aromatase,Cytochromes P450
• Solubility: DMSO:60 mg/mL (204.52 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.82 mM);Ethanol:29.3 mg/mL (99.87 mM)

Bioactivity

• Target IC50:
  Aromatase:15 nM
• In Vivo:
  Anastrozole binds to the heme group within the aromatase CYP unit, competitively inhibiting the enzyme and consequently reducing estrogen biosynthesis in breast tissue and peripheral areas. It has negligible effects on other steroid hormones. In vitro, Anastrozole exhibits high inhibitory potency, with an IC50 of 15 nM against human placental aromatase. Its efficacy is twice that of 4-OHA, 200 times that of AG, and a third of that of fadrozole.
• In Vitro:
  Administration of Anastrozole (>9.1 mg/kg) twice daily to male cynomolgus monkeys inhibits peripheral aromatase activity, reducing circulating estradiol concentrations by 50% to 60%. Oral dosing of mature rats every 2 to 3 estrous cycles with 0.1 mg/kg of Anastrozole blocks ovulation in mature female rats; administering certain doses for 3 days to pubescent rats completely inhibits uterine growth stimulated by androstenedione. These effects may be due to the suppression of the pre-ovulatory surge in estrogen synthesis within the follicles of mature female animals and the inhibition of immature ovarian metabolism of exogenous androstenedione in pubescent females.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Anastrozole, Aromatase, ZD1033, ZD-1033, ZD 1033

Compound Identifiers

PubChem CID

2187