Fludarabine(Synonyms: 氟达拉滨; F-ara-A; NSC 118218)

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Fludarabine (Synonyms: 氟达拉滨; F-ara-A; NSC 118218) 纯度: 99.85%

Fludarabine (F-ara-A; NSC 118218) 是一种 DNA 合成抑制剂和一种在淋巴增生性恶性肿瘤中具有抗肿瘤活性的氟化嘌呤类似物。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。

Fludarabine(Synonyms: 氟达拉滨; F-ara-A;  NSC 118218)

Fludarabine Chemical Structure

CAS No. : 21679-14-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
5 mg ¥500 In-stock
10 mg ¥750 In-stock
50 mg ¥2285 In-stock
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生物活性

Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes[1][2][3][4].

体外研究
(In Vitro)

Fludarabine (5 μM; 48 hours) induces a decrease in p27kip1 expression[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[4]

Cell Line: B-CLL cells
Concentration: 5 μM
Incubation Time: 24 hours
Result: Induces a decrease in p27kip1 expression. The decrease in p27kip1 expression was significantly correlated to the extent of in vitro apoptosis.

体内研究
(In Vivo)

Fludarabine (0.8 mg/kg; i.p.; two cycles for 5 days every 2 weeks) in combination with Cyclophosphamide (400 mg/kg; i.p.; 2 weeks) decreases incidence of GVHD[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: F-1 mice received 105 BCL-1 leukemia cells[5]
Dosage: 0.8 mg/kg
Administration: Intraperitoneal injection; two cycles for 5 days every 2 weeks
Result: Combination with Cyclophosphamide decreased incidence of graft-versus-host disease (GVHD).

Clinical Trial

分子量

285.23

Formula

C10H12FN5O4

CAS 号

21679-14-1

中文名称

氟达拉滨

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (87.65 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 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 1.7530 mL 3.5059 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.76 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.76 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.76 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Liang YB, et al. Downregulated SOCS1 expression activates the JAK1/STAT1 pathway and promotes polarization of macrophages into M1 type. Mol Med Rep. 2017 Nov;16(5):6405-6411.

    [2]. Sanhes L, et al. Fludarabine-induced apoptosis of B chronic lymphocytic leukemia cells includes early cleavage of p27kip1 by caspases. Leukemia. 2003 Jun;17(6):1104-11.

    [3]. Frank DA, et al. Fludarabine-induced immunosuppression is associated with inhibition of STAT1 signaling. Nat Med. 1999;5(4):444-447.

    [4]. Frank DA,et al. Fludarabine-induced immunosuppression is associated with inhibition of STAT1 signaling. Nat Med. 1999 Apr;5(4):444-7.

    [5]. Tournilhac O, et al. Impact of frontline fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cell chronic lymphocytic leukemia. Blood. 2004 Jan 1;103(1):363-5. Epub 2003 Sep 11.

    [6]. Weiss L, et al. Fludarabine in combination with cyclophosphamide decreases incidence of GVHD and maintainseffective graft-versus-leukemia effect after allogeneic stem cell transplantation in murinelymphocytic leukemia. Bone Marrow Transplant. 2003 Jan;31(1):11-5.

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