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Purity: ≥98%
Letrozole (formerly known as CGS-20267; trade name: Femara; Letoval) is a third generation, nonsteroidal inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays and has anticancer activities. As a third-generation aromatase inhibitor, letrozole inhibits aromatase selectively and reversibly, which may result in growth inhibition of estrogen-dependent breast cancer cells. Letrozole administration can reduce spine synapse and axon outgrowth and it also will decrease the expression of estrogen receptor (ER). Letrozole is proved to promote FSH release from the hypothalamic pituitary axis by responding to decreased estrogen (E) feedback. Letrozole was approved in 1996 for the treatment of local or metastatic breast cancer that is hormone receptor positive or has an unknown receptor status in postmenopausal women.
| ln Vitro |
In a dose- and time-dependent manner, letrozole (0.1–100 nM; 24-96 hours) strongly suppresses the development of MCF-7 epithelial breast cancer cells [2]. The stimulating impact of testosterone on MCF-7 cell growth is considerably inhibited by letrozole (10 nM) [2]. In MCF-7 cells, letrozole (10 nM; 24-48 hours) reduces the amounts of released metalloproteinases (MMP-2 and MMP-9) [2].
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| ln Vivo |
Rats treated with letrozole (3–300 μg/kg; once daily oral gavage for six weeks) show anti-tumor effects[3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: MCF-7 Cell Tested Concentrations: 0.1, 1, 10, 100 nM Incubation Duration: 24, 48, 96 hrs (hours) Experimental Results: Inhibition of cell growth in a dose- and time-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Adult female rats bearing mammary tumors[3]
Doses: 3, 10, 30, 100, 300 μg/kg Route of Administration: po (oral gavage) one time/day for 6 weeks Experimental Results: Induced complete regression of mammary tumors, with an ED50 of 10-30 μg/kg/day. |
| References |
[1]. Bhatnagar AS, et, al. Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. J Steroid Biochem Mol Biol. 1990 Dec 20;37(6):1021-7.
[2]. Mitropoulou TN, et, al. Letrozole as a potent inhibitor of cell proliferation and expression of metalloproteinases (MMP-2 and MMP-9) by human epithelial breast cancer cells. Int J Cancer. 2003 Mar 20;104(2):155-60. [3]. Schieweck K, et, al. Anti-tumor and endocrine effects of non-steroidal aromatase inhibitors on estrogen-dependent rat mammary tumors. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):633-6. |
| Molecular Formula |
C17H11N5
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|---|---|
| Molecular Weight |
285.3
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| CAS # |
112809-51-5
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| Related CAS # |
Letrozole-d4;1133712-96-5
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| SMILES |
N#CC1=CC=C(C(C2=CC=C(C#N)C=C2)N3N=CN=C3)C=C1
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| Chemical Name |
4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile
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| Synonyms |
Abbreviation; CGS 20267; CGS20267; CGS-20267; LTZ; Trade name: Femara; Letoval;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% CMC: 10 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5051 mL | 17.5254 mL | 35.0508 mL | |
| 5 mM | 0.7010 mL | 3.5051 mL | 7.0102 mL | |
| 10 mM | 0.3505 mL | 1.7525 mL | 3.5051 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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