Name: Bexarotene
Brand: Selleck Chemicals
SKU: S2098
Availability: InStock
Rating: 5 (19 reviews)

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Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Retinoid Receptor Inhibitors	TTNPB (Arotinoid acid) Tamibarotene AM580 Fenretinide BMS493 SR 11237 UVI 3003 AR7 Palovarotene CD1530

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (201.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.750mg/ml (5.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 35 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.862mg/ml (2.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 17.24 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	348	Formula	C₂₄H₂₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	153559-49-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LGD1069			SMILES	CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	RXR
In vitro	Bexarotene treatment at 1 mM and 10 mM for 96 h increases the number of cells with sub-G1 populations and annexin V binding in a dose-dependent manner compared with vehicle controls (DMSO) in well-established CTCL cell lines (MJ, Hut78, and HH), respectively. This compound suppresses the expression of retinoid X receptor alpha and retinoic acid receptor alpha proteins in all three lines compared with untreated controls. It decreases the protein levels of survivin, activates caspase-3, and cleaved poly(ADP-Ribose) polymerase, but has no obvious effect on expression of Fas/Fas ligand and bcl-2 proteins in all three CTCL lines. It induces a loss of viability and more pronounced inhibition of clonogenic proliferation in HH and Hut-78 cells, whereas the MJ line exhibits resistance. The chemical upregulates and activates Bax in sensitive lines, although not enough to signal significant apoptosis. It signals both G(1) and G(2)/M arrest by the modulation of critical checkpoint proteins. It activates p53 by phosphorylation at Ser15, which influences the binding of p53 to promoters for cell cycle arrest, induces p73 upregulation, and, in concordance, also modulates some p53/p73 downstream target genes, such as p21, Bax, survivin and cdc2.
In vivo	Bexarotene significantly prevents ER-negative mammary tumorigenesis with less toxicity than naturally occurring retinoids in animal models. This compound inhibits the development of preinvasive mammary lesions such as hyperplasias and carcinoma-in-situ in MMTV-erbB2 mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12006543/ [2] https://pubmed.ncbi.nlm.nih.gov/19067706/ [3] https://pubmed.ncbi.nlm.nih.gov/18362934/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-02-04)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05296304	RECRUITING	Cutaneous T-cell Lymphoma	Memorial Sloan Kettering Cancer Center	2022-03-16	PHASE1
NCT04664829	COMPLETED	Metastatic Triple-Negative Breast Carcinoma	National Cancer Centre, Singapore	2020-10-01	PHASE1
NCT05106192	WITHDRAWN	Mycosis Fungoides of Skin (Diagnosis); Cutaneous T-cell Lymphoma; Non Hodgkin Lymphoma; Lymphomatoid Papulosis; Lymphoma, Large-Cell, Anaplastic; Lymphoma, Follicular	Case Comprehensive Cancer Center	2022-04-01
NCT03323658	COMPLETED	Breast Atypical Ductal Hyperplasia; Breast Atypical Lobular Hyperplasia; Breast Ductal Carcinoma In Situ; Breast Lobular Carcinoma In Situ; Invasive Breast Carcinoma	National Cancer Institute (NCI)	2018-06-15	PHASE1
NCT03323658	Completed	Breast Atypical Ductal Hyperplasia\|Breast Atypical Lobular Hyperplasia\|Breast Ductal Carcinoma In Situ\|Breast Lobular Carcinoma In Situ\|Invasive Breast Carcinoma	National Cancer Institute (NCI)	2018-06-15	Phase 1
NCT00411632	COMPLETED	Lung Cancer	M.D. Anderson Cancer Center	2006-11-29	PHASE2

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Bexarotene Retinoid Receptor agonist

Chemical Structure

Molecular Weight: 348