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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥ 266 | 现货 | |
25 mg | ¥ 428 | 现货 | |
50 mg | ¥ 589 | 现货 | |
100 mg | ¥ 873 | 现货 | |
200 mg | ¥ 1,360 | 现货 | |
500 mg | ¥ 2,370 | 期货 | |
1 mL x 10 mM (in DMSO) | ¥ 422 | 现货 |
产品描述 | Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL). |
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。 |
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 |
别名 | 蓓萨罗丁, 贝沙罗汀, Targretin, Ro 26-4455, LGD1069 |
分子量 | 348.48 |
分子式 | C24H28O2 |
CAS No. | 153559-49-0 |
Smiles | CC1(C)C=2C(C(C)(C)CC1)=CC(C)=C(C(=C)C3=CC=C(C(O)=O)C=C3)C2 |
密度 | 1.042 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 20 mg/mL (57.39 mM), Sonication is recommended. Ethanol: 7 mg/mL (20 mM)), Heating is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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