Home Metabolism Retinoid Receptor agonist Bexarotene For research use only.

Bexarotene

Synonyms: LGD1069

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

Bexarotene Chemical Structure

Bexarotene Chemical Structure

CAS No. 153559-49-0

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Bexarotene Related Products

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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)
 June 15 2018 Phase 1
NCT01569724 Completed
Hypertriglyceridemia|Cutaneous T Cell Lymphoma
Rennes University Hospital
 January 2012 Phase 4
NCT01001143 Completed
Leukemia Myeloid Acute
Washington University School of Medicine
 May 2010 Phase 1
NCT00615784 Terminated
Acute Myeloid Leukemia
Abramson Cancer Center at Penn Medicine
 May 25 2010 Phase 2
NCT00125372 Completed
Carcinoma Non-small-cell Lung
Dartmouth-Hitchcock Medical Center|Ligand Pharmaceuticals|Genentech Inc.
 December 2005 Not Applicable
NCT00316030 Completed
AML|Acute Myeloid Leukemia
Abramson Cancer Center at Penn Medicine
 January 2004 Phase 1

Chemical Information & Solubility

Molecular Weight 348 Formula

C24H28O2
CAS No. 153559-49-0 SDF Download Bexarotene SDF
Smiles CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 69 mg/mL ( (198.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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