Bexarotene-d4 is intended for use as an internal standard for the quantification of bexarotene by GC- or LC-MS. Bexarotene is a high-affinity ligand for retinoid X receptors (RXRs) (EC50s = 28, 25, and 20 nM for RXRα, β, and γ, respectively).1 It inhibits cell cycle progression, induces apoptosis, prevents or overcomes multidrug resistance through multidrug resistance protein 1 (MDR1), and blocks angiogenesis and metastasis, making it a promising chemopreventive agent against cancer.2,3 Bexarotene also, through RXR activation, stimulates clearance of soluble β-amyloid, reduces plaque area, and reverses deficits related to Alzheimer's disease in mice.4
1.Boehm, M.F., Zhang, L., Zhi, L., et al.Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cellsJ. Med. Chem.38(16)3146-3155(1995) 2.Bischoff, E.D., Gottardis, M.M., Moon, T.E., et al.Beyond tamoxifen: The retinoid X receptor-selective ligand LGD1069 (TARGRETIN) causes complete regression of mammary carcinomaCancer Res.58(3)479-484(1998) 3.Qu, L., and Tang, X.Bexarotene: A promising anticancer agentCancer Chemother. Pharmacol.65(2)201-205(2010) 4.Cramer, P.E., Cirrito, J.R., Wesson, D.W., et al.ApoE-directed therapeutics rapidly clear β-amyloid and reverse deficits in AD mouse modelsScience335(6057)1503-1506(2012)