中文名称: | 盐酸苯达莫司汀 | ||||
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英文名称: | Bendamustine hydrochloride | ||||
别名: | 盐酸苯达莫司汀 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid hydrochloride | ||||
CAS No: | 3543-75-7 | 分子式: | C16H22Cl3N3O2 | 分子量: | 394.72 |
CAS No: | 3543-75-7 | ||||
分子式: | C16H22Cl3N3O2 | ||||
分子量: | 394.72 | ||||
MDL: | MFCD01658758 | EINEC: | 1864 | ||
EINEC: | 1864 |
基本信息
产品编号:B10779 |
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产品名称:Bendamustine hydrochloride |
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CAS: |
3543-75-7 |
储存条件 |
粉末 |
2-8℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
394.72 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
78mg/mL (197.6mM) |
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Ethanol |
78mg/mL (197.6mM) |
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Water |
78mg/mL (197.6mM) |
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体内(现配现用) |
1% DMSO+30% polyethylene glycol+1% Tween 80 |
30mg/mL |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.5334mL |
12.6672mL |
25.3344mL |
5mM |
0.5067mL |
2.5334mL |
5.0669mL |
10mM |
0.2533mL |
1.2667mL |
2.5334mL |
50mM |
0.0507mL |
0.2533mL |
0.5067mL |
生物活性
产品描述 |
一种嘌呤类似物,是一种 DNA 交联剂。 |
靶点/IC50 |
DNA synthesis |
体外研究 |
Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.Bendamustine uniquely regulates apoptosis pathways and DNA repair pathways in non-Hodgkin's lymphoma cells.Bendamustine (50μM) induces p21 (Cip1/Waf1) and NOXA genes, and increases the expression of p53 in SU-DHL-1 cells.Bendamustine (25μM) blocks mitotic checkpoints and cuases mitotic catastrophe.Bendamustine reduces the viability of multiple myeloma (MM) cell lines, such as RPMI-8226 and 8226-LR5 cells, with IC25s of 101.8μM and 585.5μM after 24h incubation, and 51.7 and 374.3μM after 48h incubation,respectively.Bendamustine induces a specific caspase-dependent MM cell death and inhibits the spindle-assembly checkpoint. |
体内研究 |
Bendamustine (25mg/kg, i.v.) shows potent inhibition on the growth of tumor cells by 91%, 99% and 95% for DoHH-2,Granta 519 and RAMOS models, respectively. Moreover, the antitumor effect of Bendamustine is enhanced by rituximab in DoHH-2 and RAMOS models, but not in Granta 519 model. |
推荐实验方法(仅供参考)
细胞实验: |
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Cytotoxicity of both Bendamustine and melphalan on multiple myeloma (MM) cells is calculated as inhibition of cell viability by measuring the percentage of cell survival by MTS assay. Briefly,cells (1 × 104/well) are seeded in 96-well plates with increasing concentrations of the drug and analyzed after 24, 48, 72 and 96h of incubation. To this end, 1μg/mL of MTS solution is added to each well and, after 1 h at 37℃, the dark blue formazan crystals are dissolved by isopropanol 1N and HCl (24:1, vol/vol). Finally, the absorbance is measured at 490nm in a 96-well plate reader.Cell survival is estimated as the percentage of the absorbance of untreated controls and each test is performed in triplicate. The inhibitory concentrations 50 (IC50) and 25 (IC25) of each drug, being the amount able to reduce cell growth to 50% and 25%, respectively, of that of untreated control cells, are calculated, and the tests are performed in parallel using equitoxic concentrations of Bendamustine and melphalan. The relative resistance index (RRI) is expressed as the ratio of the IC50 of 8226-LR5 to the IC50 of RPMI-8226 cells. |
动物实验: |
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Mice C.B.-17 scid mice (DoHH-2, Granta 519) or C.B.-17 scid-bg mice (SuDHL-4, RAMOS) are inoculated with 1 × 106 (DoHH-2,RAMOS),3×106 (SuDHL-4) or 5 × 106 (Granta 519) cells s.c. in the right flank. For flank xenografts, inoculation volume is 0.2mL consisting of a 50:50 mixture of cells in growth medium and Matrigel.Tumour volume is estimated by two to three weekly measurements of the length and width of the tumour by electronic calipers and applying the following equation:V=L×W2/2. Tumours are allowed to reach approximately 250mm3, and mice are size-matched (day 0) into treatment and control groups. For systemic Granta 519 tumour models, 2 × 106 cells are injected via the tail vein in 0.1mL volume of cell medium on day 0,and treatment is initiated on day 14. All animals are ear-tagged and monitored individually throughout the experiment. Navitoclax is administered by oral gavage once daily in a mixture of Phosal 50PG : PEG400 : ethanol.Bendamustine and rituximab are administered i.v. at 25mg/kg and 10mg/kg,respectively,on day 1. Navitoclax is administered approximately 2h before Bendamustine and rituximab. All trials are comprised of 10mice per group. Mice are humanely killed when tumours reach a size >2000 mm3 or when any signs of distress are monitored. Signs of distress include loss of ambulation, laboured breathing or weight loss > 20% mean body weight per cage. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )