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Bexarotene

Catalog No. T6410Cas No. 153559-49-0
Alias Targretin, Ro 26-4455, LGD1069

Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).

Bexarotene

Bexarotene

Purity: 99%
Catalog No. T6410Alias Targretin, Ro 26-4455, LGD1069Cas No. 153559-49-0
Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).
Pack SizePriceAvailabilityQuantity
10 mg$30In Stock
25 mg$44In Stock
50 mg$62In Stock
100 mg$91In Stock
200 mg$123In Stock
500 mg$261In Stock
1 mL x 10 mM (in DMSO)$39In Stock
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Purity:99%
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Product Introduction

Bioactivity
Description
Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).
In vitro
Bexarotene inhibited the expression of retinoid X receptor alpha and retinoic acid receptor alpha proteins in CTCL cell lines (MJ,HUT78 and 11 h).1 mM and 10 mM Bexarotene treatment of CTCL cell lines (MJ,HUT78 and 11 h) for 96 h increased cellular sub-G1 populations and membrane-bound protein V binding in a dose-dependent manner. Bexarotene treatment reduced the levels of surviving proteins, activated caspase-3 and cleaved poly (ADP-ribose) polymerase, but had no significant effect on the expression of Fas/Fas ligand and bcl-2 proteins in all three CTCL lines.Bexarotene induced a loss of viability and a more pronounced inhibition of clone formation in HH and Hut-78 cells proliferation, while the MJ line showed resistance.
In vivo
Bexarotene inhibited the expression of retinoid X receptor alpha and retinoic acid receptor alpha proteins in CTCL cell lines (MJ,HUT78 and 11 h).1 mM and 10 mM Bexarotene treatment of CTCL cell lines (MJ,HUT78 and 11 h) for 96 h increased cellular sub-G1 populations and membrane-bound protein V binding in a dose-dependent manner. Bexarotene treatment reduced the levels of surviving proteins, activated caspase-3 and cleaved poly (ADP-ribose) polymerase, but had no significant effect on the expression of Fas/Fas ligand and bcl-2 proteins in all three CTCL lines.Bexarotene induced a loss of viability and a more pronounced inhibition of clone formation in HH and Hut-78 cells proliferation, while the MJ line showed resistance.
Kinase Assay
Biacore studies: Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~ 200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel
AliasTargretin, Ro 26-4455, LGD1069
Chemical Properties
Molecular Weight348.48
FormulaC24H28O2
Cas No.153559-49-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 20 mg/mL (57.39 mM), Sonication is recommended.
Ethanol: 7 mg/mL (20 mM)), Heating is recommended.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.8696 mL14.3480 mL28.6961 mL143.4803 mL
5 mM0.5739 mL2.8696 mL5.7392 mL28.6961 mL
10 mM0.2870 mL1.4348 mL2.8696 mL14.3480 mL
20 mM0.1435 mL0.7174 mL1.4348 mL7.1740 mL
DMSO
1mg5mg10mg50mg
50 mM0.0574 mL0.2870 mL0.5739 mL2.8696 mL

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