Bexarotene 是一种高亲和力的选择性类视黄醇 X 受体 (RXR) 激动剂，对RXRα、RXRβ和RXRγ的EC50分别为 33、24和25 nM。它是一种类视黄醇类似物，用于治疗皮肤 T 细胞淋巴瘤的皮肤表现。

Bexarotene is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).

Bexarotene抑制MMTV-erbB2的小鼠中浸润前乳腺病变,如增生和癌的发展.Bexarotene明显预防动物模型中ER阴性乳腺肿瘤形成,毒性比天然存在的类视色素更低.

Bexarotene抑制CTCL细胞系（MJ,HUT78和11 h）中类视黄醇X受体α和视黄酸受体α蛋白的表达。1 mM和10 mM Bexarotene处理CTCL细胞系（MJ,HUT78和11 h）中96小时,以剂量依赖性方式增加细胞亚G1群和膜联蛋白V结合。Bexarotene处理减少存活的蛋白水平,活化的caspase-3和切割的聚（ADP-核糖）聚合酶,但对所有三种CTCL系中Fas/Fas配体和bcl-2蛋白的表达没有明显影响。Bexarotene在HH和Hut-78细胞中诱导活力丧失和更显著抑制克隆形成增殖,而MJ系表现出抗性。

Biacore studies: Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~ 200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel

153559-49-0

C24H28O2

348.486

Targretin;贝沙罗汀;Ro 26-4455;LGD1069;蓓萨罗丁

Ethanol:7 mg/mL (20 mM)),with gentle warming
DMSO:34.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years