Bexarotene (LGD1069)

Catalog No.S2098 Synonyms: Targretin

For research use only.

Bexarotene (Targretin, LGD1069) is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.

Bexarotene (LGD1069) Chemical Structure

CAS No. 153559-49-0

Selleck's Bexarotene (LGD1069) has been cited by 11 Publications

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Purity & Quality Control

Choose Selective Retinoid Receptor Inhibitors

Biological Activity

Description Bexarotene (Targretin, LGD1069) 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)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 348
Formula

C24H28O2

CAS No. 153559-49-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C

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

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03323658 Active not recruiting Drug: Bexarotene|Other: Questionnaire Administration 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 Other: oral glucose tolerance test (OGTT) Hypertriglyceridemia|Cutaneous T Cell Lymphoma Rennes University Hospital January 2012 Phase 4
NCT01001143 Completed Drug: Decitabine|Drug: Bexarotene Leukemia Myeloid Acute Washington University School of Medicine May 2010 Phase 1
NCT00615784 Terminated Drug: Bexarotene Acute Myeloid Leukemia Abramson Cancer Center of the University of Pennsylvania May 25 2010 Phase 2
NCT00125372 Completed Drug: erlotinib (Tarceva) and bexarotene (Targretin) Carcinoma Non-small-cell Lung Dartmouth-Hitchcock Medical Center|Ligand Pharmaceuticals|Genentech Inc. December 2005 Not Applicable
NCT00316030 Completed Drug: Bexarotene AML|Acute Myeloid Leukemia Abramson Cancer Center of the University of Pennsylvania January 2004 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

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