Bexarotene
产品名称:Bexarotene
产品描述:
产品描述 | Bexarotene 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, LGD1069, 贝沙罗汀, Targretin, Ro 26-4455 |
分子量 | 348.49 |
分子式 | C24H28O2 |
CAS No. | 153559-49-0 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 34.9 mg/mL (100 mM)
Ethanol: 7 mg/mL (20 mM)),with gentle warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发,涵盖生物科技、化学品、中间体和化工材料等领域。
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