氟达拉滨|T1038|TargetMol

Fludarabine
21679-14-1

￥183 1mg 起订

￥397 5mg 起订

￥619 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 氟达拉滨

英文名称：: Fludarabine

CAS号：: 21679-14-1

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.88%

产品类别：: 抑制剂

货号：: T1038

Product Introduction

Bioactivity

名称	Fludarabine
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.
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].
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]
存储条件	store at low temperature,keep away from direct sunlight,keep away from moisture \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 55 mg/mL (192.83 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.85 mg/mL (9.99 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字	Nucleoside Antimetabolite/Analog \| Fludarabine \| purine analogue \| STAT1 \| NSC-118218 \| DNA/RNA Synthesis \| Apoptosis \| Inhibitor \| fluorinated \| lymphoproliferative malignancies \| STAT \| NSC118218 \| inhibit
相关产品	Guanidine hydrochloride \| L-Glutamic acid \| Metronidazole \| 5-Fluorouracil \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Tributyrin \| L-Ascorbic acid \| Acetylcysteine \| Salicylic acid \| Thymidine \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌上市药物库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 抗衰老化合物库 \| 抗病毒库 \| FDA 上市药物库 \| 抗癌临床化合物库 \| 抗癌药物库

氟达拉滨|||氟达拉宾|||NSC 118218|||Fludarabinum|||F-ara-A|TargetMol

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