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.
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Bexarotene Chemical Structure
CAS No. : 153559-49-0
This product is a controlled substance and not for sale in your territory.
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.
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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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.
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
ConcentrationSolventMass
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
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.
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
Protocol 3
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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 4
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
[1]. Nathalia Rodrigues de Almeida, et al. A review of the molecular design and biological activities of RXR agonists. Med Res Rev. 2019 Jul;39(4):1372-1397.
[Content Brief]
[2]. Danyang Shen, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer. Onco Targets Ther. 2019 Sep 24;12:7877-7886.
[Content Brief]
[3]. Y Wang, et al. Prevention of lung cancer progression by bexarotene in mouse models. Oncogene. 2006 Mar 2;25(9):1320-9.
[Content Brief]
[1]. Nathalia Rodrigues de Almeida, et al. A review of the molecular design and biological activities of RXR agonists. Med Res Rev. 2019 Jul;39(4):1372-1397.
[2]. Danyang Shen, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer. Onco Targets Ther. 2019 Sep 24;12:7877-7886.
[3]. Y Wang, et al. Prevention of lung cancer progression by bexarotene in mouse models. Oncogene. 2006 Mar 2;25(9):1320-9.
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
ConcentrationSolventMass
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
Bexarotene Related Classifications
Metabolic Enzyme/ProteaseVitamin D Related/Nuclear ReceptorAutophagy
RAR/RXRAutophagy
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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