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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

348.48

C₂₄H₂₈O₂

153559-49-0

贝沙罗汀；蓓萨罗丁

Room temperature in continental US; may vary elsewhere.

DMSO : 60 mg/mL (172.18 mM; Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

  Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

  Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic
• 3.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.97 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 4.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.97 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 5.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.97 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.

  [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.

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