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Fludarabine

产品编号 T1038 CAS 21679-14-1

别名: NSC 118218, Fludarabinum, 氟达拉宾, 氟达拉滨, F-ara-A

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。

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Fludarabine, CAS 21679-14-1

规格	价格/CNY	货期
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

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其他形式的 Fludarabine:

Fludarabine triphosphate
询价

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纯度: 100%

纯度: 99.88%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 28.5 mg/mL (100 mM)

溶液配制表

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

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Meng H, et al. Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo. Eur J Haematol. 2007 Dec;79(6):486-93. 2. Torella D, et al. Fludarabine prevents smooth muscle proliferation in vitro and neointimal hyperplasia in vivo through specific inhibition of STAT-1 activation. Am J Physiol Heart Circ Physiol. 2007 Jun;292(6):H2935-43. 3. Weiss L, 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. Bone Marrow Transplant. 2003 Jan;31(1):11-5. 4. Zhu Y, Gu H, Yang L, et al. The sequential role of Mst1/mTORC1/STAT1 activity in chemokine receptor 2-regulated B cell receptor signaling[J]. Authorea Preprints. 2021 5. Wang S, He F, Li Z, et al. Long non-coding RNA BANCR promotes interferon-β-induced cardiomyocyte apoptosis by targeting signal transducer and activator of transcription 1 in vitro[J]. International Journal of Clinical and Experimental Pathology. 2020, 13(11): 2840. 6. Chu K H, Lin S Y, Chiang B L. STAT6 Pathway Is Critical for the Induction and Function of Regulatory T Cells Induced by Mucosal B Cells[J]. Frontiers in immunology. 2020, 11. 7. Chen C, Lu M, Lin S, et al. The nuclear gene rpl18 regulates erythroid maturation via JAK2-STAT3 signaling in zebrafish model of Diamond–Blackfan anemia[J]. Cell Death & Disease. 2020, 11(2): 1-11. 8. Yang L, Li N, Yang D, et al. CCL2 regulation of MST1-mTOR-STAT1 signaling axis controls BCR signaling and B-cell differentiation[J]. Cell Death & Differentiation. 2021: 1-18.

文献引用

1. Yang L, Li N, Yang D, et al. CCL2 regulation of MST1-mTOR-STAT1 signaling axis controls BCR signaling and B-cell differentiation. Cell Death & Differentiation. 2021: 1-18 2. Wang X, Li X, Wang J, et al. SMGL-1/NBAS acts as a RAB-8 GEF to regulate unconventional protein secretion. Journal of Cell Biology. 2022, 221(7): e202111125 3. Zhang T, Wang Y, Li Q, et al. Mesenchymal stromal cells equipped by IFNα empower T cells with potent anti-tumor immunity. Oncogene. 2022: 1-16. 4. Zhu Y, Gu H, Yang L, et al. Involvement of MST1/mTORC1/STAT1 activity in the regulation of B-cell receptor signalling by chemokine receptor 2. Clinical and Translational Medicine. 2022, 12(7): e887. 5. Chen C, Lu M, Lin S, et al. The nuclear gene rpl18 regulates erythroid maturation via JAK2-STAT3 signaling in zebrafish model of Diamond–Blackfan anemia. Cell Death & Disease. 2020, 11(2): 1-11 6. Chu K H, Lin S Y, Chiang B L. STAT6 Pathway Is Critical for the Induction and Function of Regulatory T Cells Induced by Mucosal B Cells. Frontiers in immunology. 2021 Jan 29;11:615868. doi: 10.3389/fimmu.2020.615868. eCollection 2020. 7. Wang S, He F, Li Z, et al. Long non-coding RNA BANCR promotes interferon-β-induced cardiomyocyte apoptosis by targeting signal transducer and activator of transcription 1 in vitro. International Journal of Clinical and Experimental Pathology. 2020, 13(11): 2840. 8. Ye S, Li S, Qin L, et al.GBP2 promotes clear cell renal cell carcinoma progression through immune infiltration and regulation of PD‑L1 expression via STAT1 signaling.Oncology Reports.2023, 49(3): 1-14. 9. Zhang X, Wang J, Wang M, et al.IFN-β Pretreatment Alleviates Allogeneic Renal Tubular Epithelial Cell–Induced NK Cell Responses via the IRF7/HLA-E/NKG2A Axis.The Journal of Immunology.2023 10. Zhang J, Guo H, Wang L, et al.Cediranib enhances the transcription of MHC-I by upregulating IRF-1.Biochemical Pharmacology.2024: 116036.

11. Lu X, Ji Q, Pan H, et al.IL-23p19 deficiency reduces M1 macrophage polarization and improves stress-induced cardiac remodeling by alleviating macrophage ferroptosis in mice.Biochemical Pharmacology.2024: 116072. 12. Zeng L, Lyu X, Yuan J, et al.STMN1 Promotes Tumor Metastasis in Non-small Cell Lung Cancer Through Microtubule-dependent And Nonmicrotubule-dependent Pathways.International Journal of Biological Sciences.2024, 20(4): 1509.

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

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。

Keywords

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

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Fludarabine

存储

溶解度

溶液配制表

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参考文献

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剂量换算

体内实验配液计算器

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