Bexarotene - CAS 153559-49-0
Catalog number:
153559-49-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C24H28O2
Molecular Weight:
348
COA:
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Targets:
RAR/RXR
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.
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Purity:
>98%
Synonyms:
LGD1069
MSDS:
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1. Combination of photodynamic therapy and immunomodulation for skin diseases-update of clinical aspects
Xiu-Li Wang, Hong-Wei Wang, Kai-Hua Yuan, Fu-Lun Li and Zheng Huang*. Photochem. Photobiol. Sci., 2011, 10, 704
Generally speaking, low-dose combination therapy may improve treatment safety and tolerability. A combination of PUVA and immune response modifier (e.g. interferon a (IFNα)-subcutaneously 3 times a week to the maximal tolerable dosage or bexarotene – orally 75–300 mg day-1) in early disease has been showntobeeffectiveandwelltolerated.IFNa and bexarotene target not only the pathogenic T-cells (e.g. direct antiproliferative effects) but can also correct the immune dysregulation in CTCL by supporting cytotoxic Th1 immune responses. In advanced stages of CTCL, extracorporeal photopheresis may be combined with IFNa or bexarotene to correct the immune dysregulation inCTCL by restoring normal equilibrium of Th1 cells. Reduced doses of these combinations, including the application of topical PDT, may also be effective as maintenance therapies following complete remission, but the durability of response and impact on overall survival remains to be determined.
2. Electron densities of bexarotene and disila-bexarotene from invariom application: a comparative study
Peter Luger,* Manuela Weber, Christian Hübschleb and Reinhold Tacke*. Org. Biomol. Chem., 2013, 11, 2348–2354
The retinoid X receptor (RXR) agonist bexarotene (1a, Targretin®) is in clinical use for the treatment of cutaneous T-cell lymphoma (Fig. 1). Recently, this agent raised additional attention in that therapeutic effects on Alzheimer’s disease in mouse models were discussed. Disila-bexarotene (1b), a silicon analogue of bexarotene (1a), was also shown to be a highly potent RXR agonist (Fig. 1), and a series of structurally related C/Si analogues were demonstrated to be very potent retinoid agonists as well. For a deeper understanding of pharmacological activities on an atomic scale, not only the geometric but also the electronic properties of the drug molecule should be examined. In the case of the C/Si analogues bexarotene (1a) and disila-bexarotene (1b), carbon and silicon differ not only in their covalent radii but also in their electronegativities. Therefore, considerable differences in the electronic properties, for example in the electrostatic potentials (ESPs), can be expected for 1a and 1b. Knowledge of these ESPs could be very helpful in characterising the pharmacological properties of these two compounds.
3. Folate-modified bexarotene-loaded bovine serum albumin nanoparticles as a promising tumor-targeting delivery system
Lisi Qi, Yuanyuan Guo, Jingjing Luan, Dianrui Zhang, Zhongxi Zhao and Yuxia Luan*. J. Mater. Chem. B,2014, 2,8361–8371
Bexarotene (BEX, also known as Targretin), (Fig. 1) a synthetic retinoid X receptor-selective activator, has been proved to be an efficacious chemopreventive and chemotherapeutic agent. As a suppressor of carcinogenesis, bexarotene can inhibit growth and induce differentiation and apoptosis in many different cancer cell lines including the prostate cancer breast cancer cell and lung cancer cell. It has been demonstrated to be extremely effective in inhibiting non-small cell lung cancer (NSCLC) and successfully used in the treatment of cutaneous T-cell lymphomas and lymphomatoid papulosis, showing promising inhibitory effects on mammary tumors and ER-negative breast cancer. Nevertheless, bexarotene is poorly water-soluble, with a maximum solubility of about 10–50 mMin pure water, resulting in poor bioavailability and limited applications. Moreover, results from recent clinical trials in patients with advanced lung cancer or breast cancer have not demonstrated significant activities of bexarotene, suggesting further modification of the drug delivery system. As a consequence, there remains a need to find novel drug vehicles to extend its clinical administration.
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CAS 153559-49-0 Bexarotene

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