2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy
  3. RAR/RXR Autophagy
  4. Bexarotene

Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.

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

Bexarotene Chemical Structure

Bexarotene Chemical Structure

CAS No. : 153559-49-0

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
50 mg USD 79 In-stock
100 mg USD 119 In-stock
500 mg USD 383 In-stock
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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of Bexarotene:

Bexarotene Related Antibodies

Top Publications Citing Use of Products

    Bexarotene purchased from MedChemExpress. Usage Cited in: Neurobiol Dis. 2018 Sep;117:114-124.  [Abstract]

    Bexarotene increases neuronal maintenance and inhibits cell apoptosis after controlled cortical impact (CCI). Representative Western blotting images of cleaved caspase-3, Bax and Bcl-2 in ipsilateral brain on the 14th day after CCI.

    Bexarotene purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016;40(5):1239-1251.  [Abstract]

    Arithmetic means±SEM (n=14) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) bexarotene (0.2-0.6 µg/mL). For comparison, the effect of the solvent DMSO is shown (grey bar).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM)[1][2][3]. Bexarotene can be used for the research of cutaneous T-cell lymphoma.

    In Vitro

    Bexarotene selectively binds and activates RXR subtypes with Kd=14±2 nM, 21±4 nM, and 29±7 nM for RXRα, RXRβ, and RXRγ subtypes[1].
    Bexarotene is effective in limiting the proliferation of leukemic (HL-60) cells. Bexarotene inhibits the proliferation of HL-60 cells by 37% at 1 μM[1].
    Bexarotene monotherapy of cells shows an antiproliferative effect at a high dose, and the IC50s aere 40.62±0.45 μM (PC3) and 50.20±4.10 μM (DU145)[2].
    Bexarotene (20 and 40 μM) and Docetaxel (5 and 10 μM) exhibit a synergistic effect on the inhibition of PC3 and DU145 cell proliferation[2].
    Bexarotene (20 and 40 μM) represses cyclin D1 and cyclin D3 expression in PC3 and DU145 cells[2].

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

    Bexarotene Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: The human PCa androgen-independent cell lines PC3 and DU145
    Concentration: 5, 10, 20, 30, 40 μM for PC3 cells; 1, 5, 10, 20, 40 μM for DU145 cells.
    Incubation Time: 24 and 48 hours
    Result: Showed an antiproliferative effect with the IC50s were 40.62±0.45 µM (PC3) and 50.20±4.10 µM (DU145). 

    Cell Viability Assay[2]

    Cell Line: PC3 and DU145 cells
    Concentration: 20 and 40 µM
    Incubation Time: 24 or 48 hours
    Result: Decreased cyclin D1, and cyclin E2 after 24 hours treatment. 
    Not only decreased the expression of cyclin D1 and cyclin E2 but repressed cyclin B1 and CDK1 expression after 48 hours treatment.
    In Vivo

    Bexarotene (1 mg/kg/day) is effective in blocking the development of behavioral deficits and dopamine neuron degeneration in a rat model of Parkinson’s disease (PD) producing significantly reduced changes in both triglycerides and T4 serum[1].
    Bexarotene is an effective preventive agent against lung tumor growth and progression. Bexarotene (100 mg/kg by gavage) inhibits both tumor multiplicity and tumor volume in mice of all three genotypes (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt). Bexarotene reduces the progression of adenoma to adenocarcinoma by ～50% in both p53wt/wtK-rasko/wt and p53wt/wtK-raswt/wt mice[3].

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

    Animal Model: UL53-3 mice (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt)[3]
    Dosage: 100 mg/kg
    Administration: Gavage with 18 gage of gavage-needle, 0.1 mL per mouse per day, 5 times a week, continued for 12 weeks
    Result: Inhibited both tumor multiplicity and tumor volume in mice of all three genotypes.
    Clinical Trial
    Molecular Weight

    348.48

    Formula

    C24H28O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1(C2=C(C(C)(CC1)C)C=C(C(C(C3=CC=C(C=C3)C(O)=O)=C)=C2)C)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 60 mg/mL (172.18 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 2.8696 mL 14.3480 mL 28.6961 mL
    5 mM 0.5739 mL 2.8696 mL 5.7392 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic

    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: 99.92%

    COA (251 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8696 mL 14.3480 mL 28.6961 mL 71.7401 mL
    5 mM 0.5739 mL 2.8696 mL 5.7392 mL 14.3480 mL
    10 mM 0.2870 mL 1.4348 mL 2.8696 mL 7.1740 mL
    15 mM 0.1913 mL 0.9565 mL 1.9131 mL 4.7827 mL
    20 mM 0.1435 mL 0.7174 mL 1.4348 mL 3.5870 mL
    25 mM 0.1148 mL 0.5739 mL 1.1478 mL 2.8696 mL
    30 mM 0.0957 mL 0.4783 mL 0.9565 mL 2.3913 mL
    40 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7935 mL
    50 mM 0.0574 mL 0.2870 mL 0.5739 mL 1.4348 mL
    60 mM 0.0478 mL 0.2391 mL 0.4783 mL 1.1957 mL
    80 mM 0.0359 mL 0.1794 mL 0.3587 mL 0.8968 mL
    100 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7174 mL
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    Bexarotene Related Classifications

    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.

    Keywords:

    Bexarotene153559-49-0LGD1069LGD 1069LGD-1069RAR/RXRAutophagyRetinoic acid receptorsRetinoid X receptorsselective,?retinoidRXRcutaneousT-celllymphomaantineoplasticanti-cancerInhibitorinhibitorinhibit

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