Bexarotene (Synonyms: LGD1069)

Name: Bexarotene
Brand: MedChemExpress
SKU: HY-14171
Rating: 5.0 (21 reviews)

Cat. No.: HY-14171 Purity: 99.92%: FAQs
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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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 87	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 383	In-stock	Estimated Time of Arrival: December 31
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Based on 21 publication(s) in Google Scholar

Other Forms of Bexarotene:

Bexarotene-d₄ Get quote
Bexarotene-d3 Get quote
Bexarotene (Standard) Get quote

19 Publications Citing Use of MCE Bexarotene

Proliferation Assay

: 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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RXRα RXRβ RXRγ

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.

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	26.5 μM Compound: Bexarotene	Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
A-375	IC₅₀	28.4 μM Compound: Bexarotene	Cytotoxicity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
BT-549	EC₅₀	> 56 μM Compound: Bex	Cytotoxicity against human BT549 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human BT549 cells assessed as reduction in cell viability by MTT assay	[PMID: 29287960]
Caco-2	EC₅₀	52 nM Compound: 1, Bexarotene	Agonist activity at human recombinant Gal4-tagged RXRalpha expressed in human Caco-2 cells assessed as receptor homodimerization after 24 hrs by mammalian two hybrid assay Agonist activity at human recombinant Gal4-tagged RXRalpha expressed in human Caco-2 cells assessed as receptor homodimerization after 24 hrs by mammalian two hybrid assay	[PMID: 19791803]
COS-1	EC₅₀	20 nM Compound: Bexarotene	Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay	[PMID: 25815156]
COS-1	EC₅₀	20 nM Compound: 1, LGD1069	Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay	[PMID: 24900241]
CV-1	EC₅₀	0.04 μM Compound: 37, LGD1069	Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at after 6 hrs by Dual-light chemiluminescent assay Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at after 6 hrs by Dual-light chemiluminescent assay	[PMID: 19216008]
DU-145	IC₅₀	61.6 μM Compound: bexarotene	Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707260]
FaDu	IC₅₀	29.8 μM Compound: Bexarotene	Cytotoxicity against human FaDu cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human FaDu cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
HEK293	EC₅₀	149 nM Compound: bexarotene	Transactivation of human RXRalpha transfected in human 293 cells after 48 hrs by dual-luciferase reporter gene assay Transactivation of human RXRalpha transfected in human 293 cells after 48 hrs by dual-luciferase reporter gene assay	[PMID: 23707260]
HEK293	EC₅₀	40 nM Compound: Targretin, Bexarotene	Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay	[PMID: 24801499]
HEK-293T	EC₅₀	0.196 μM Compound: 18	Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	0.434 μM Compound: 18	Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
Hep 3B2	IC₅₀	191.8 μM Compound: bexarotene	Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707260]
HepG2	IC₅₀	20 μM Compound: 2	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by WST-1 assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by WST-1 assay	[PMID: 33793232]
HGC-27	IC₅₀	32.7 μM Compound: bexarotene	Cytotoxicity against human HGC27 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HGC27 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707260]
HT-29	IC₅₀	> 30 μM Compound: Bexarotene	Cytotoxicity against human HT29 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human HT29 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
KB	IC₅₀	46.3 μM Compound: bexarotene	Cytotoxicity against bexarotene-resistant human KB cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against bexarotene-resistant human KB cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23707260]
KB	IC₅₀	8.8 μM Compound: bexarotene	Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707260]
MCF7	IC₅₀	10.6 μM Compound: Bexarotene	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
MDA-MB-231	EC₅₀	> 56 μM Compound: Bex	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by MTT assay	[PMID: 29287960]
NIH3T3	IC₅₀	18.7 μM Compound: Bexarotene	Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 32422522]
Sf9	IC₅₀	13.5 μM Compound: 40	Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]
Sf9	IC₅₀	5.9 μM Compound: 40	Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase	[PMID: 26918322]

In Vitro

Bexarotene selectively binds and activates RXR subtypes with K_d=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.

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 (p53^wt/wtK-ras^wt/wt, p53^val135/wtK-ras^wt/wt, or p53^wt/wtK-ras^ko/wt). Bexarotene reduces the progression of adenoma to adenocarcinoma by ～50% in both p53^wt/wtK-ras^ko/wt and p53^wt/wtK-ras^wt/wt mice^[3].

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

Animal Model:	UL53-3 mice (p53^wt/wtK-ras^wt/wt, p53^val135/wtK-ras^wt/wt, or p53^wt/wtK-ras^ko/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.

153559-49-0

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
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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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
Protocol 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

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 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

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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

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 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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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%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (251 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

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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Bexarotene (Synonyms: LGD1069)

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Other Forms of Bexarotene:

Bexarotene Related Antibodies

19 Publications Citing Use of MCE Bexarotene

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•Related Screening Libraries:

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View All RAR/RXR Isoform Specific Products:

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References

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Bexarotene Related Antibodies

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Complete Stock Solution Preparation Table

Bexarotene Related Classifications

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