Letrozole

SKU: orb1308084

Description

Letrozole

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 112809-51-5
• MW: 285.3
• Purity: 99.75%
• Formula: C₁₇H₁₁N₅
• SMILES: N#CC1=CC=C(C=C1)C(N1C=NC=N1)C1=CC=C(C=C1)C#N
• Target: Cytochromes P450,Aromatase,Autophagy
• 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 inhibit 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 concentration up to 50 μM. In rat adrenal tissue stimulated by ACTH (Adrenocorticotropic Hormone), letrozole suppresse 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 o the growth of tumors formed by MCF-7 cells, which have been transfected wit 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 concentration of Letrozole are added. A 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.
• 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