Fludarabine
(Synonyms: 氟达拉滨; F-ara-A; NSC 118218) 目录号 : GC14144
Fludarabine是一种抑制DNA合成的嘌呤类似物。
Cas No.:21679-14-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | MEC-2 cells、Flu-resistant clonal cells |
Preparation Method | Cells were treated with or without 100µM Fludarabine for 72h and cell viability was analyzed by MTT. |
Reaction Conditions | 100μM; 72h |
Applications | Fludarabine induces MEC-2 cells apoptosis but not flu-resistant clonal cells. |
| Animal experiment [2]: | |
Animal models | B-cell leukemia (BCL-1) bearing (BALB/c×C57BL/6) F1 mice |
Preparation Method | Mice received 105 BCL-1 leukemic cells and 1 day later were given 0.8mg/kg Fludarabine intraperitoneally for 5 consecutive days. 2 weeks later, mice received another 5-day cycle of 0.8mg/kg Fludarabine and 2 weeks later received 400mg/kg cyclophosphamide intraperitoneally. Control animals received saline instead of fludarabine. One day after cyclophosphamide treatment, C57BL/6 precursor cells were transplanted and the development of leukemia and the extent of graft-versus-host disease (GVHD) were monitored clinically and histopathologically. |
Dosage form | 0.8mg/kg, two cycles for 5 days every 2 weeks; i.p. |
Applications | Fludarabine in combination with cyclophosphamide decreases incidence of GVHD and maintains effective graft-versus-leukemia effect after allogeneic stem cell transplantation in murine lymphocytic leukemia. |
References: | |
Fludarabine is a purine analog that inhibits DNA synthesis[1]. Fludarabine inhibits cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal quiescent or activated lymphocytes[2]. Fludarabine is an anti-tumor agent used to treat leukemia and lymphoma[3].
In vitro, treatment of MEC-2 cells with Fludarabine (100μM) for 72h significantly reduced cell viability, induced cytochrome c release and DNA cleavage[4]. Treatment of chronic lymphocytic leukemia (CLL) cells with Fludarabine (3, 10, 30μM) for 24-72h induced apoptosis in a dose- and time-dependent manner, increased intracellular phosphorylation of H2A histone family member X (H2AX), and led to DNA damage[5].
In vivo, treatment of BCL-1-bearing F1 mice with Fludarabine (0.8mg/kg) by intraperitoneal injection reduced the incidence of graft-versus-host disease (GVHD) in mice and maintained the anti-leukemic effect after leukemic cell transplantation[6]. Treatment of SCID beige mice with Fludarabine (200mg/kg) by intraperitoneal injection for 6 weeks promoted the engraftment of acute myeloid leukemia (AML) cell lines[7].
References:
[1] Wang Y, Chen X, Tang N, et al. Boosting Clear Cell Renal Carcinoma-Specific Drug Discovery Using a Deep Learning Algorithm and Single-Cell Analysis[J]. International Journal of Molecular Sciences, 2024, 25(7): 4134.
[2] Battle T E, Frank D A. STAT1 mediates differentiation of chronic lymphocytic leukemia cells in response to Bryostatin 1[J]. Blood, 2003, 102(8): 3016-3024.
[3] Ricci F, Tedeschi A, Morra E, et al. Fludarabine in the treatment of chronic lymphocytic leukemia: a review[J]. Therapeutics and clinical risk management, 2009: 187-207.
[4] Huang C, Tu Y, Freter C E. Fludarabine-resistance associates with ceramide metabolism and leukemia stem cell development in chronic lymphocytic leukemia[J]. Oncotarget, 2018, 9(69): 33124.
[5] El-Mabhouh A A, Ayres M L, Shpall E J, et al. Evaluation of bendamustine in combination with fludarabine in primary chronic lymphocytic leukemia cells[J]. Blood, The Journal of the American Society of Hematology, 2014, 123(24): 3780-3789.
[6] Weiss L, Abdul-Hai A, Or R, et al. Fludarabine in combination with cyclophosphamide decreases incidence of GVHD and maintains effective graft-versus-leukemia effect after allogeneic stem cell transplantation in murine lymphocytic leukemia[J]. Bone marrow transplantation, 2003, 31(1): 11-15.
[7]Pievani A, Michelozzi I M, Rambaldi B, et al. Fludarabine as a cost-effective adjuvant to enhance engraftment of human normal and malignant hematopoiesis in immunodeficient mice[J]. Scientific RepoRts, 2018, 8(1): 9125.
Fludarabine是一种抑制DNA合成的嘌呤类似物[1]。Fludarabine抑制细胞因子诱导的正常静止或激活淋巴细胞中STAT1和STAT1依赖性基因转录的激活[2]。Fludarabine是一种抗肿瘤剂，用于治疗白血病和淋巴瘤[3]。
在体外，Fludarabine（100μM）处理MEC-2细胞72h，显著降低了细胞的活力，诱导了细胞色素c释放和DNA裂解[4]。Fludarabine（3、10、30μM）处理慢性淋巴细胞白血病（CLL）24-72h，剂量和时间依赖性地诱导了细胞凋亡，增加了细胞内H2A组蛋白家族成员X（H2AX）磷酸化，导致了DNA损伤[5]。
在体内，Fludarabine（0.8mg/kg）通过腹膜内注射治疗B型淋巴细胞白血病（BCL-1）携带F1小鼠，降低了小鼠移植物抗宿主病（GVHD）的发生率，并在白血病细胞移植后保持了抗白血病作用[6]。Fludarabine（200mg/kg）通过腹腔注射治疗SCID beige小鼠6周，促进了急性髓系白血病（AML）细胞系的植入[7]。
| Cas No. | 21679-14-1 | SDF | |
| 别名 | 氟达拉滨; F-ara-A; NSC 118218 | ||
| 化学名 | (2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol | ||
| Canonical SMILES | C1=NC2=C(N1C3C(C(C(O3)CO)O)O)N=C(N=C2N)F | ||
| 分子式 | C10H12FN5O4 | 分子量 | 285.23 |
| 溶解度 | ≥ 9.25mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5059 mL | 17.5297 mL | 35.0594 mL |
| 5 mM | 0.7012 mL | 3.5059 mL | 7.0119 mL |
| 10 mM | 0.3506 mL | 1.753 mL | 3.5059 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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