Bexarotene

Catalog No.S2098 Batch:S209806

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Technical Data

Formula

C24H28O2
Molecular Weight 348 CAS No. 153559-49-0
Solubility (25°C)* In vitro DMSO 69 mg/mL (198.27 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.75mg/ml 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 95% Corn oil
0.862mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.
Targets
RXR [1]
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. Bexarotene treatment suppresses the expression of retinoid X receptor alpha and retinoic acid receptor alpha proteins in all three lines compared with untreated controls. Bexarotene treatment 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. [1] Bexarotene induces a loss of viability and more pronounced inhibition of clonogenic proliferation in HH and Hut-78 cells, whereas the MJ line exhibits resistance. Bexarotene upregulates and activates Bax in sensitive lines, although not enough to signal significant apoptosis. Bexarotene signals both G(1) and G(2)/M arrest by the modulation of critical checkpoint proteins. Bexarotene 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. [2]
In vivo Bexarotene significantly prevents ER-negative mammary tumorigenesis with less toxicity than naturally occurring retinoids in animal models. Bexarotene inhibits the development of preinvasive mammary lesions such as hyperplasias and carcinoma-in-situ in MMTV-erbB2 mice. [3]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , Neurol Res, 2018, 40(8):702-708]

Selleck's Bexarotene has been cited by 16 publications

Whitening of brown adipose tissue inhibits osteogenic differentiation via secretion of S100A8/A9 [ iScience, 2024, 27(2):108857] PubMed: 38303710
Tretinoin synergistically enhances the antitumor effect of combined BRAF, MEK, and EGFR inhibition in BRAFV600E colorectal cancer [ Cancer Sci, 2024, 10.1111/cas.16280] PubMed: 39175203
GZ17-6.02 interacts with bexarotene to kill mycosis fungoides cells [ Oncotarget, 2024, 15:124-133] PubMed: 38329728
Chromatin accessibility dynamics dictate renal tubular epithelial cell response to injury [ Nat Commun, 2022, 13(1):7322] PubMed: 36443310
Targeting the TR4 nuclear receptor with antagonist bexarotene can suppress the proopiomelanocortin signalling in AtT-20 cells [ J Cell Mol Med, 2021, 10.1111/jcmm.16074] PubMed: 33491272
Targeting the TR4 nuclear receptor with antagonist bexarotene can suppress the proopiomelanocortin signalling in AtT-20 cells [ J Cell Mol Med, 2021, 25(5):2404-2417] PubMed: 33491272
Effect of propylene glycol on the skin penetration of drugs [ Arch Dermatol Res, 2020, 312(5):337-352] PubMed: 31786711
The support of genetic evidence for cardiovascular risk induced by antineoplastic drugs [ Sci Adv, 2020, 6(42)eabb8543] PubMed: 33055159
[ Nat Metab, 2019, ] PubMed: 31984309
Activation of retinoid X receptor by bexarotene attenuates neuroinflammation via PPARγ/SIRT6/FoxO3a pathway after subarachnoid hemorrhage in rats. [ J Neuroinflammation, 2019, 16(1):47] PubMed: 30791908

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.