名称 | Carmustine |
描述 | Carmustine (bis-chloroethylnitrosourea) is a cell-cycle phase nonspecific alkylating antineoplastic agent. |
激酶实验 | The determination of Acetyl-CoAdependent N-acetylation of 2-aminofluorene (AF) and p-aminobenzoic acid (PABA) are performed. Incubation mixtures in the assay system consists of a total volume of 90 μL: glial tumor cells cytosols, diluted as required, in 50 μL of lysis buffer (20 mM Tris/HCl, pH 7.5, 1 mM DTT and 1 mM EDTA), 20 μL of an Acetyl-CoA recycling mixture of 50 mM Tris-HCl (pH7.5), 0.2 mM EDTA, 2 mM DTT, 15 mM acetylcamitine, 2U/mL carnitine acetyltransferase, and AF or PABA at specific concentrations. The reactions are started by addition of 20 μL of Acetyl-CoA. The control reactions have 20 μL distilled water in place of Acetyl-CoA. For the single point activity measurements, the final concentration of AF or PABA is 0.1 mM and AcCoA is 0.5 mM. The reaction mixtures with or without specific concentrations of Carmustine and lomustine are incubated at 37°C for 10 min and stopped with 50 μL of 20% trichloroacetic acid for the PABA reactions, and 100 μL of acetonitrile for the AF reactions. All of the reactions (experiments and controls) are run in triplicate |
动物实验 | Carmustine is formulated in corn oil.RatsIndividual rats are weighted prior to enter the study; their weights are recorded, and they are randomLy assigned to four groups. Group I (saline group); This group consists of 12 rats. These rats are injected with 2 mL/kg of saline intraperitoneally (IP) 48 h before the study, being included by the study 48 h later. Group II (corn oil group) consists of 15 rats. These rats are injected with 2 mL/kg of corn oil (vehicle) IP 48 h before the study. Group III (Carmustine group) consists of 16 rats. These rats are injected with 1 mL per day of saline IP, administered at the same hour of the day as a single-dose for 3 days. Twelve hours after the first dose of saline, corn oil 2 mL/kg + Carmustine 25 mg/kg IP are injected, and the rats are included in the study 48 h after the administration of corn oil + Carmustine. Group IV (trimetazidine group) consists of 12 rats. These rats are injected with 2.5 mg/kg per day of trimetazidine (TMZ) IP, administered at the same hour of the day as a single-dose for 3 days. 12 h after the first dose of TMZ, corn oil 2 mL/kg + Carmustine 25 mg/kg IP are injected, and the rats are included in the study 48 h after the administration of corn oil + Carmustine |
体外活性 | Carmustine 是一种抗肿瘤化合物。在浓度为 8, 80, 和 800 μM 时,Carmustine 降低了大鼠神经胶质瘤细胞质和完整细胞中对2-氨基荧光素(AF)和对氨基苯甲酸(PABA)的N-乙酰转移酶(NAT)活性。同时,Carmustine 减少了DNA-AF 加合物的形成,尽管在大鼠神经胶质瘤细胞中DNA-AF 加合物的含量有所增加。 |
体内活性 | Carmustine (BCNU;25 mg/kg,腹腔注射)在实验鼠中引起的肝重比(肝脏重量与体重的比值)和血浆结合胆红素水平均高于对照组,而胆汁流量、氧化型谷胱甘肽(GSSG)水平以及还原型谷胱甘肽(GSH)/GSSG比值则低于对照组。 |
存储条件 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 55 mg/mL (256.95 mM)
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关键字 | Carmustine | DNA Alkylator/Crosslinker | Inhibitor | inhibit |
相关产品 | Methyl methanesulfonate | Ifosfamide | Cisplatin | N-Nitroso-N-methylurea | Streptozocin | Temozolomide | Busulfan | Oxaliplatin | Cyclophosphamide hydrate | Cyclophosphamide | Carboplatin | Bendamustine hydrochloride |
相关库 | 抗癌活性化合物库 | 抗癌上市药物库 | 经典已知活性库 | EMA 上市药物库 | 抗衰老化合物库 | FDA 上市药物库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 抗癌药物库 |