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Endocrinology/Hormones Aromatase Letrozole

Letrozole

Catalog No. T1590   CAS 112809-51-5
Synonyms: CGS 20267

Letrozole is an Aromatase Inhibitor. The mechanism of action of letrozole is as an Aromatase Inhibitor.

Letrozole, CAS 112809-51-5
Pack Size Availability Price/USD Quantity
25 mg In stock 44.00
50 mg In stock 55.00
100 mg In stock 66.00
200 mg In stock 74.00
500 mg In stock 86.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description Letrozole is an Aromatase Inhibitor. The mechanism of action of letrozole is as an Aromatase Inhibitor.
Targets&IC50 Aromatase : ic50 0.07nM-20nM,  
Kinase Assay Human placental aromatase activity: The assay is performed in a total volume of 1 mL at 37 ℃. Unless otherwise noted, the incubation mixture contains 11 nM [4- 14C] androstene-3, 17-dione ([4- 14C]A), 24 mM NADPH (tetrasodium salt Type III), the appropriate concentrations of the desired inhibitor, and 120 μg of microsomal protein. The (4- 14C)A is added as a solution in 1.7% ethanol in 0.05 M potassium phosphate buffer (pH 7.4), so that the final concentration of ethanol does not exceed 0.02% (v/v). The reaction is started by the addition of enzyme and stopped after 20 min by the addition of 7 vol of ethyl acetate. The mixture is agitated on a vortex mixer and centrifuged at 600 g for 5 min. The aqueous phase is re-extracted with 7 vol of ethyl acetate, and the combined extracts are evaporated to dryness using an Evapo-Mix. Over 99% of the radio- active of [4- 14C] added is recovered using this extraction system. The residue obtained is dissolved in 150 μL acetone, and 100 μL aliquots are chromatographed for 65 min on thin-layer plates precoated with silica gel 60 using ethyl: acetate: isooctane (140:60, v/v; system A) or toluene: chloroform: methanol (70:140:20; system B). The radioactive zones of the plate are located with a Berthold LB 2760 thin-layer scanner. The radioactive estradiol (E2) and estrone (E1) neaks are identified by comparison with authentic standards. The corresponding bonding band of silica gel is transferred to vials containing 10 mL of scintillation fluid, and counted with a 6880 Liquid Scintillation system.
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)
Cell lines: Human breast cancer cells MCF-7
Animal Research
Animal Model: Human breast carcinoma xenografts MCF-7 with human aromatase gene (MCF-7Ca)
Synonyms CGS 20267
Purity 99.68%
Molecular Weight 285.3
Formula C17H11N5
CAS No. 112809-51-5

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 28.5 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

0.5% CMC: 10 mg/mL

Citations

References and Literature
1. Haynes BP, et al. J Steroid Biochem Mol Biol, 2003, 87(1), 35-45. 2. Bhatnagar AS, et al. J Steroid Biochem Mol Biol, 1990, 37(6), 1021-1027. 3. Mitropoulou TN, et al. Int J Cancer, 2003, 104(2), 155-160. 4. Dellapasqua S, et al. Expert Opin Drug Metab Toxicol, 2010, 6(2), 251-259. 5. Lee K, et al. Int J Cancer, 1995, 62(3), 297-302.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Autophagy Compound Library Endocrinology-Hormones Library FDA-approved Drug Library Anti-cancer Approved drug Library

Related Products

Related compounds with same targets
Anastrozole Androsta-1,4,6-triene-3,17-dione Formestane Aminoglutethimide Org30958 Exemestane Letrozole 3,4-Dimethoxyhydrocinnamic acid

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