Bexarotene  (Synonyms: LGD1069)

Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC₅₀s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC₅₀ >10000 nM)^[1][2][3]. Bexarotene can be used for the research of cutaneous T-cell lymphoma.

Bexarotene?selectively binds and activates RXR subtypes with K_d=14±2 nM, 21±4 nM, and 29±7 nM for RXRα, RXRβ, and RXRγ subtypes^[1].?
Bexarotene?is effective in limiting the proliferation of leukemic (HL-60) cells.?Bexarotene inhibits the proliferation of HL-60 cells by 37% at 1 μM^[1].??
Bexarotene monotherapy of cells shows an antiproliferative effect at a high dose, and the IC₅₀s aere 40.62±0.45?μM (PC3) and 50.20±4.10?μM (DU145)^[2].??
Bexarotene (20 and 40 μM) and Docetaxel (5 and 10 μM) exhibit a synergistic effect on the inhibition of PC3 and DU145 cell proliferation^[2].
Bexarotene (20 and 40?μM) represses cyclin D1 and cyclin D3 expression in PC3 and DU145 cells^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Bexarotene??(1 mg/kg/day) is effective in blocking the development of behavioral deficits and dopamine neuron degeneration in a rat model of Parkinson’s disease (PD) producing significantly reduced changes in both triglycerides and T4 serum^[1].?
Bexarotene is an effective preventive agent against lung tumor growth and progression. Bexarotene (100?mg/kg by gavage) inhibits both tumor multiplicity and tumor volume in mice of all three genotypes (p53^wt/wtK-ras^wt/wt, p53^val135/wtK-ras^wt/wt, or p53^wt/wtK-ras^ko/wt). Bexarotene reduces the progression of adenoma to adenocarcinoma by?～50% in both p53^wt/wtK-ras^ko/wt?and p53^wt/wtK-ras^wt/wt?mice^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

348.48

Solid

C₂₄H₂₈O₂

153559-49-0

CC1(C2=C(C(C)(CC1)C)C=C(C(C(C3=CC=C(C=C3)C(O)=O)=C)=C2)C)C

Room temperature in continental US; may vary elsewhere.

• [1]. Nathalia Rodrigues de Almeida, et al.  A review of the molecular design and biological activities of RXR agonists. Med Res Rev. 2019 Jul;39(4):1372-1397.  [Content Brief]

  [2]. Danyang Shen, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer. Onco Targets Ther. 2019 Sep 24;12:7877-7886.  [Content Brief]

  [3]. Y Wang, et al. Prevention of lung cancer progression by bexarotene in mouse models. Oncogene. 2006 Mar 2;25(9):1320-9.  [Content Brief]