Letrozole

SKU: orb1226953

Description

Letrozole (INN, trade name Femara) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant treatment of hormonally-responsive breast Y Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. (In Vitro):Letrozole (0.1-100 nM; 24-96 h) significantly inhibits growth of the MCF-7 epithelial breast cancer cells in a dose- and time-dependent manner.Letrozole (10 nM) significantly suppresses the stimulatory effects of testosterone on MCF-7 cell proliferation.Letrozole (10 nM; 24-48 h) suppresses the levels of secreted metalloproteinases (MMP‐2 and MMP‐9) in MCF-7 cells(In Vivo):Letrozole (3-300 μg/kg; oral gavage once daily for 6 weeks) exhibits anti-tumor effects in rats.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 112809-51-5
• MW: 285.3
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₁N₅
• SMILES: N#CC1=CC=C(C(C2=CC=C(C#N)C=C2)N3N=CN=C3)C=C1
• Target: Aromatase
• Solubility: DMSO: 57 mg/mL (199.78 mM)

Bioactivity

• In Vivo:
  Letrozole (3-300 μg/kg; oral gavage once daily for 6 weeks) exhibits anti-tumor effects in rats. Animal model: Adult female rats bearing mammary tumors. Dosage: 3, 10, 30, 100, 300 μg/kg. Administration: Oral gavage once daily for 6 weeks. Result: Induced complete regression of mammary tumors, with an ED50 of 10-30 μg/kg/day.
  Read more...
• In Vitro:
  Letrozole (0.1-100 nM; 24-96 h) significantly inhibits growth of the MCF-7 epithelial breast cancer cells in a dose- and time-dependent manner. Letrozole (10 nM) significantly suppresses the stimulatory effects of testosterone on MCF-7 cell proliferation. Letrozole (10 nM; 24-48 h) suppresses the levels of secreted metalloproteinases (MMP‐2 and MMP‐9) in MCF-7 cells. Cell Viability Assay Cell line: MCF-7 cells. Concentration: 0.1, 1, 10, 100 nM Incubation time: 24, 48, 96 hours. Result: Inhibited cells growth in a dose- and time-dependent manner.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CGS 20267

Quick Database Links

Gene Symbol

Aromatase