product name Bexarotene
Description: Bexarotene, also known as LGD-1069, is a synthetic retinoid selective for retinoid X receptors, it is used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma. Bexarotene selectively binds to and activates retinoid X receptors, thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, apoptosis of some cancer cell types, and tumor regression.
References: Clin Cancer Res. 2002;8(5):1234-40; Br J Dermatol. 2009;160(3):519-26; Br J Cancer. 2008;98(8):1380-8.
348
Formula
C24H28O2
CAS No.
153559-49-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 8 mg/mL (23.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
LGD1069
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Cancer Res. 2002 May;8(5):1234-40; Br J Dermatol. 2009 Mar;160(3):519-26; Br J Cancer. 2008 Apr 22;98(8):1380-8. |
