1. Metabolic Enzyme/Protease
    Autophagy
  2. RAR/RXR
    Autophagy
  3. Bexarotene

Bexarotene (Synonyms: LGD1069)

Cat. No.: HY-14171 Purity: 99.81%
Handling Instructions

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

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10 mM * 1 mL in DMSO USD 87 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Bexarotene:

Top Publications Citing Use of Products

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

    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).

    Bexarotene purchased from MCE. Usage Cited in: Neurobiol Dis. 2018 Sep;117:114-124.

    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.
    • Biological Activity

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    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].

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

    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].

    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.
    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)

    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
    10 mM 0.2870 mL 1.4348 mL 2.8696 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

    • 4.

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

      Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

    • 5.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

    *All of the co-solvents are available by MCE.
    References

    Purity: 99.90%

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