Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fludarabine (Fludarabinum) 是一种氟化嘌呤类似物,一种核酸合成抑制剂和 STAT1 激活抑制剂。Fludarabine 具有抗肿瘤活性,可以用于治疗白血病和淋巴瘤。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 397 | 现货 | ||
10 mg | ¥ 624 | 现货 | ||
50 mg | ¥ 1,914 | 现货 | ||
100 mg | ¥ 2,751 | 现货 | ||
200 mg | ¥ 3,852 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 398 | 现货 |
产品描述 | Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma. |
体外活性 |
方法:多发性骨髓瘤细胞 RPMI8226、MM.1S 和 MM.1R 用 Fludarabine (0-64 µg/mL) 处理 24-48 h,使用 MTT Assay 检测细胞活力。 结果:Fludarabine 剂量-时问依赖性抑制 RPMI8226 细胞增殖,24 h 的 IC50 为 1.54 µg/mL。48 h,Fludarabine 对MM.1S 和 MM.1R 细胞的 IC50 分别为 13.48 µg/mL 和 33.79 µg/mL。[1] 方法:大鼠主动脉 VSMCs 用 Fludarabine (50 µM) 和 FBS 处理 30 min,使用 Western Blot 检测靶点蛋白表达水平. 结果:FBS 刺激产生了渐进的 JAK2 和 STAT-1 激活,Fludarabine 诱导 STAT-1 磷酸化的显著减少,而它没有改变 JAK2 的激活。[2] |
体内活性 |
方法:为检测体内抗肿瘤活性,将 Fludarabine (8-40 mg/kg) 腹腔注射给携带多发性骨髓瘤 RPMI8226 的 SCID 小鼠,每天一次,持续三天。 结果:与对照肿瘤中的约 10 倍相比,用 40mg/kg 的 Fludarabine 治疗的肿瘤在 25 天内增加了不到 5 倍,证明了 Fludarabine 在体内的抗肿瘤活性。[1] 方法:为研究对移植物抗宿主病 (GVHD) 的作用,将 Fludarabine (0.8 mg/kg) 腹腔注射给携带 B 细胞白血病 (BCL-1) 的 (BALB/c x C57BL/6)F1 小鼠,每两周接受两个周期的给药五天,然后腹腔注射 cyclophosphamide (400 mg/kg)。 结果:在移植前用含 Fludarabine 的方案治疗的小鼠在临床和尸检中的 GVHD 也少得多,而移植物抗白血病似乎在相同的动物中增加。[3] |
细胞实验 | VSMCs were isolated from the aorta of male Wistar rats weighing ~350–500 g, as previously described. For cell culture experiments, 2 × 10^5 rat VSMCs were plated in Dulbecco's modified Eagle's medium (DMEM) with 10% fetal bovine serum (FBS). Semiconfluent VSMCs were starved by incubation in 0.5% FBS/DMEM for 36–48 h and then serum-stimulated with normal growth medium (i.e., DMEM containing 10% FBS) in the presence or absence of fludarabine (50 μM) [2]. |
动物实验 | The animals in this study were handled according to the animal welfare regulation of the Magna Graecia University of Catanzaro, and the protocol was approved by the animal use committee of this institution. Fifty Wistar rats weighing 340 ± 40 g were anesthetized with an intramuscular injection of 100 mg/kg ketamine and 5 mg/kg xylazine. Angioplasty of the common carotid artery was performed using a balloon embolectomy catheter, as previously described and well validated in our laboratory. Fludarabine was dissolved in 30% pluronic F127 gel to the final concentrations of 2.5, 5, 15, or 25 mg/ml. At the time of balloon injury, gel containing fludarabine or vehicle was applied around the middle segment (2 cm in length) of the right injured carotid artery (0.1 ml per 1-cm length of the artery segment, equivalent to 0.5, 1, 3, or 5 mg of total fludarabine locally delivered), as previously described. As a control experiment, 200 μl of fludarabine/gel solution (25 mg/ml) were applied around the sham-operated carotid artery. To study the fludarabine toxicity, laboratory studies were performed at baseline and 2 wk after drug local delivery (25 mg/ml). Arterial pressure and heart rate were measured indirectly by a tail-cuff plethysmographic technique [2]. |
别名 | NSC 118218, Fludarabinum, 氟达拉宾, 氟达拉滨, F-ara-A |
分子量 | 285.23 |
分子式 | C10H12FN5O4 |
CAS No. | 21679-14-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 28.5 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.5059 mL | 17.5297 mL | 35.0594 mL | 87.6486 mL |
5 mM | 0.7012 mL | 3.5059 mL | 7.0119 mL | 17.5297 mL | |
10 mM | 0.3506 mL | 1.753 mL | 3.5059 mL | 8.7649 mL | |
20 mM | 0.1753 mL | 0.8765 mL | 1.753 mL | 4.3824 mL | |
50 mM | 0.0701 mL | 0.3506 mL | 0.7012 mL | 1.753 mL | |
100 mM | 0.0351 mL | 0.1753 mL | 0.3506 mL | 0.8765 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Fludarabine 21679-14-1 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair JAK/STAT signaling Stem Cells Nucleoside Antimetabolite/Analog DNA/RNA Synthesis STAT purine analogue STAT1 NSC-118218 NSC 118218 Fludarabinum 氟达拉宾 Inhibitor 氟达拉滨 fluorinated F-ara-A lymphoproliferative malignancies NSC118218 inhibit inhibitor