Letrozole

SKU: orb1308084

Description

Letrozole (CGS 20267) is a potent, non-steroidal aromatase inhibitor. It is widely used in research to study estrogen-dependent processes, including investigations into breast cancer models both in vitro and in vivo.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 112809-51-5
• MW: 285.3
• Purity: 99.84% (May vary between batches)
• Formula: C₁₇H₁₁N₅
• SMILES: N#CC1=CC=C(C=C1)C(N1C=NC=N1)C1=CC=C(C=C1)C#N
• Target: Autophagy,Aromatase,Cytochromes P450
• Solubility: DMSO:245 mg/mL (858.75 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.01 mM)

Bioactivity

• Target IC50:
  Aromatase:0.07 nM-20 nM
• In Vivo:
  Letrozole inhibits the production of estradiol in hamster ovarian tissue induced by LH (Luteinizing Hormone), with an IC50 of 0.02 μM, and does not significantly affect progesterone production at concentrations up to 350 μM. In rat adrenal tissue stimulated by ACTH (Adrenocorticotropic Hormone), letrozole suppresses the production of aldosterone, with an IC50 of 210 μM. In non-cellular systems, its IC50 ranges from 1-13 nM. Letrozole effectively inhibits aromatase activity derived from various sources, including human placental microsomes, human breast cancer particulate fractions, rat ovarian microsomes, MCF-7 cells transfected with aromatase, JEG-3 choriocarcinoma cells, CHO (Chinese Hamster Ovary) cells, hamster ovarian tissue, and human breast cancer particulate fractions, with respective IC50 values of 11, 2, 7, 0.07, 0.07, 1.4, 20, and 0.8 nM.
• In Vitro:
  Letrozole exhibits a dose-dependent inhibitory effect on the growth of tumors formed by MCF-7 cells, which have been transfected with the human aromatase gene (MCF-7Ca), in athymic nude mice. It completely inhibits tumor growth at a dosage of 20 mg/kg/day. In vivo studies have demonstrated that Letrozole can suppress aromatase activity, with an oral ED50 of 1-3 μg/mg.
• Cell Research:
  Cells are seeded in duplicate at 5,000 to 10,000 cells per well in 24-well plates. The day after plating, different concentrations of Letrozole are added. At the end of incubation, cells are trypsinizated and placed in Isotone solution and counted immediately using a Coulter particle-counter. (Only for Reference)

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

CGS 20267, CGS20267, CGS-20267, breast, Aromatase, Autophagy, cancer, estrogen, Inhibitor, Letrozole, inhibit

Compound Identifiers

PubChem CID

3902