1. Metabolic Enzyme/Protease Autophagy
  2. Cytochrome P450 Autophagy
  3. Letrozole

Letrozole  (Synonyms: CGS 20267)

Cat. No.: HY-14248 Purity: 99.95%
COA Handling Instructions

Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.

For research use only. We do not sell to patients.

Letrozole Chemical Structure

Letrozole Chemical Structure

CAS No. : 112809-51-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 87 In-stock
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Solid
100 mg USD 79 In-stock
200 mg USD 85 In-stock
500 mg USD 100 In-stock
1 g   Get quote  
5 g   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of Letrozole:

Top Publications Citing Use of Products

    Letrozole purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2018 Jun;15(6):5269-5274.  [Abstract]

    Letrozole significantly increases the protein levels of Ras/ERK1/c-Myc in the classical MAPK pathway.

    Letrozole purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2018 Jun;15(6):5269-5274.  [Abstract]

    Detection of the effects of Letrozole and the MAPK pathway on the proliferation of GC-1 spg cells by BrdU. MAPK, mitogen-activated protein kinase; spg, spermatogonia; BrdU, bromodeoxyuridine.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer[1][2][3].

    IC50 & Target

    Aromatase

     

    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[2].
    Letrozole (10 nM) significantly suppresses the stimulatory effects of testosterone on MCF-7 cell proliferation[2].
    Letrozole (10 nM; 24-48 h) suppresses the levels of secreted metalloproteinases (MMP‐2 and MMP‐9) in MCF-7 cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[2]

    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.
    In Vivo

    Letrozole (3-300 μg/kg; oral gavage once daily for 6 weeks) exhibits anti-tumor effects in rats[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Adult female rats bearing mammary tumors[3]
    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.
    Clinical Trial
    Molecular Weight

    285.30

    Formula

    C17H11N5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    N#CC1=CC=C(C(N2C=NC=N2)C3=CC=C(C#N)C=C3)C=C1

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (175.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.95%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.5051 mL 17.5254 mL 35.0508 mL 87.6271 mL
    5 mM 0.7010 mL 3.5051 mL 7.0102 mL 17.5254 mL
    10 mM 0.3505 mL 1.7525 mL 3.5051 mL 8.7627 mL
    15 mM 0.2337 mL 1.1684 mL 2.3367 mL 5.8418 mL
    20 mM 0.1753 mL 0.8763 mL 1.7525 mL 4.3814 mL
    25 mM 0.1402 mL 0.7010 mL 1.4020 mL 3.5051 mL
    30 mM 0.1168 mL 0.5842 mL 1.1684 mL 2.9209 mL
    40 mM 0.0876 mL 0.4381 mL 0.8763 mL 2.1907 mL
    50 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7525 mL
    60 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4605 mL
    80 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
    100 mM 0.0351 mL 0.1753 mL 0.3505 mL 0.8763 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Letrozole
    Cat. No.:
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