For research use only.
Catalog No.S2098 Synonyms: Targretin, LGD1069
CAS No. 153559-49-0
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.
Selleck's Bexarotene has been cited by 8 publications
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Bexarotene inhibited microglia activation after SAH. Left, Representative immunofluorescent images of Iba1 (red) and DAPI (blue) in basal cortex at 24 h after SAH (N = 4/group, mean ± SD). Scale bar, 30 μm. Right, quantification of Iba1 positive cells per mm2. ***p < 0.001 compared with the Sham group, ###p < 0.001 compared with the SAH + vehicle group.
Neurol Res, 2018, 40(8):702-708. Bexarotene purchased from Selleck.
Purity & Quality Control
Choose Selective Retinoid Receptor Inhibitors
|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.|
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.  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. 
|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. |
|In vitro||DMSO||8 mg/mL (22.98 mM)|
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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||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|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|
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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