Bexarotene

Catalog No.S2098 Synonyms: LGD1069

Bexarotene Chemical Structure

Molecular Weight(MW): 348

Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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Choose Selective Retinoid Receptor Inhibitors

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

Solubility (25°C)

In vitro DMSO 8 mg/mL (22.98 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 348
Formula

C24H28O2

CAS No. 153559-49-0
Storage powder
Synonyms LGD1069

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02061878 Completed Alzheimers Disease ReXceptor, Inc. August 2014 Phase 1
NCT01782742 Completed Alzheimers Disease The Cleveland Clinic February 2013 Phase 2
NCT01578499 Active, not recruiting Primary Cutaneous Anaplastic Large Cell Lymphoma|Mycosis Fungoides|Cutaneous T-Cell Lymphoma Millennium Pharmaceuticals, Inc.|Seattle Genetics, Inc.|Takeda August 2012 Phase 3
NCT01504490 Terminated Solid Tumors|Lymphoma|Multiple Myeloma Georgetown University|Daiichi Sankyo Inc. December 2011 Phase 1
NCT01001143 Completed Leukemia, Myeloid, Acute Washington University School of Medicine May 2010 Phase 1
NCT01134341 Completed Cutaneous T-cell Lymphoma|Mycosis Fungoides|Sezary Syndrome|Primary Cutaneous Anaplastic Large Cell Lymphoma Spectrum Pharmaceuticals, Inc March 2010 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID