贝沙罗汀 T6410

Product Introduction
Bioactivity


英文名: Bexarotene

描述: Bexarotene (LGD1069) 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。

激酶实验: 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

体外活性: 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.

体内活性: 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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 20 mg/mL (57.39 mM)
Ethanol : 7 mg/mL (20 mM))


关键字: cutaneous | lymphoma | selective,?retinoid | inhibit | Retinoic acid receptors | antineoplastic | Bexarotene | LGD 1069 | LGD-1069 | T-cell | RAR/RXR | Inhibitor | anti-cancer | Retinoid X receptors | RXR | Autophagy

相关产品: AR7 | AGN 196996 | Bigelovin | LE135 | AGN 192870 | BMS493 | UVI 3003 | Tarenflurbil | palovarotene | Magnolol

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Nuclear Receptor Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途