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抑制剂/激动剂
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/ Fludarabine

氟达拉滨 /Fludarabine 98%

货号：A175546 同义名： 氟达拉宾 / F-ara-A;NSC 118218 Ambeed 开学季，买赠积分，赢豪礼

Fludarabine(NSC 118218) 是一种 DNA 合成抑制剂和氟化嘌呤类似物，在淋巴增殖性恶性肿瘤中具有抗肿瘤活性。它抑制细胞因子诱导的 STAT1 激活及其在正常静止或活化淋巴细胞中的依赖 STAT1 的基因转录。

Fludarabine 化学结构 CAS号：21679-14-1
Fludarabine 化学结构
CAS号：21679-14-1
Fludarabine 3D分子结构
CAS号：21679-14-1
Fludarabine 化学结构 CAS号：21679-14-1
Fludarabine 3D分子结构 CAS号：21679-14-1
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Fludarabine 纯度/质量文件 产品仅供科研

货号：A175546 标准纯度： 98%
批次查询： 批次纯度:

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产品名称 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 98%
Favipiravir ✔ 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

 		98%
SU056 +

YB-1, IC50: 1.73 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Fludarabine 生物活性

靶点

  • STAT1
描述 Fludarabine (2-F-ARAA, 2-fluoro ARA-A) is a chemotherapy drug used in the treatment of chronic lymphocytic leukemia (see https://www.fda.gov/) for targeting on DNA synthesis. It can also work as an inhibitor of STAT1 activation. The mechanism of Fludarabine action against to DNA synthesis is similar to other nucleotide analogues. Fludarabine can be phosphorylated to form as the Fludarabine triphosphate and then compete with natural nucleotides to inhibit DNA polymeraseα and incorporate into DNA strand. It can also act on ribonucleotide reductase and thus deplete the dATP pool[1]. Fludarabine can also cause a specific depletion of STAT1, but not of other STATs, as well as cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in lymphocytes[2].
作用机制 Fludarabine can inhibit DNA synthesis through targeting to ribonucleotide reductase and DNA polymerase.

Fludarabine 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
624.38mel 50 μM Function Assay 24 h decreases IDO expression 24911872
624.38mel 50-200 μM Function Assay 24 h inhibits IDO activity independently of mRNA levels 24911872
A549 Growth Inhibition Assay IC50=15.7±2.8 µM 23377192
A549 Growth Inhibition Assay IC20=5.48 × 10−8 μM  18661380

Fludarabine 动物研究

Dose Mice (i.p.): min = 0.3 mg/kg[4], max = 200 mg/kg[5]
Administration i.p.
Pharmacokinetics
Animal Mice[6] Rats[6] Dogs[6]
Dose 40 mg/m3 120 mg/m3 86.7 mg/m2
Administration i.v. i.v.
p.o. 		i.v.
p.o.
T1/2 1.9 h 3.3 h (i.v.)
3.1 h (p.o.) 		2.0 h (i.v.)
1.9 h (p.o.)
Vss 0.061 L 0.8 L 7.65 L
F 0.81 1.008
Tmax 1.0 h (p.o.) 0.6 h (p.o.)
AUC 66.1 μM·hr (p.o.) 46.6 μM·hr (p.o.)
Cmax 9.9 μM (p.o.) 4.39 μM (p.o.)
CLsp 0.37 ml/min 2.75 ml/min 44.5 ml/min

Fludarabine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00006251 Acute Undifferentiated Leukemi... 展开 >>a Adult Nasal Type Extranodal NK/T-cell Lymphoma Anaplastic Large Cell Lymphoma Angioimmunoblastic T-cell Lymphoma Childhood Burkitt Lymphoma Childhood Diffuse Large Cell Lymphoma Childhood Grade III Lymphomatoid Granulomatosis Childhood Immunoblastic Large Cell Lymphoma Childhood Myelodysplastic Syndromes Childhood Nasal Type Extranodal NK/T-cell Lymphoma Chronic Myelomonocytic Leukemia Cutaneous B-cell Non-Hodgkin Lymphoma de Novo Myelodysplastic Syndromes Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue Hepatosplenic T-cell Lymphoma Intraocular Lymphoma Juvenile Myelomonocytic Leukemia Mast Cell Leukemia Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable Myeloid/NK-cell Acute Leukemia Nodal Marginal Zone B-cell Lymphoma Noncutaneous Extranodal Lymphoma Peripheral T-cell Lymphoma Post-transplant Lymphoproliferative Disorder Previously Treated Myelodysplastic Syndromes Primary Systemic Amyloidosis Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Recurrent Adult Burkitt Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Adult Diffuse Mixed Cell Lymphoma Recurrent Adult Diffuse Small Cleaved Cell Lymphoma Recurrent Adult Grade III Lymphomatoid Granulomatosis Recurrent Adult Hodgkin Lymphoma Recurrent Adult Immunoblastic Large Cell Lymphoma Recurrent Adult Lymphoblastic Lymphoma Recurrent Adult T-cell Leukemia/Lymphoma Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Recurrent Childhood Anaplastic Large Cell Lymphoma Recurrent Childhood Grade III Lymphomatoid Granulomatosis Recurrent Childhood Large Cell Lymphoma Recurrent Childhood Lymphoblastic Lymphoma Recurrent Childhood Small Noncleaved Cell Lymphoma Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Recurrent Mycosis Fungoides/Sezary Syndrome Recurrent Renal Cell Cancer Recurrent Small Lymphocytic Lymphoma Recurrent/Refractory Childhood Hodgkin Lymphoma Refractory Chronic Lymphocytic Leukemia Refractory Hairy Cell Leukemia Refractory Multiple Myeloma Small Intestine Lymphoma Splenic Marginal Zone Lymphoma Stage II Multiple Myeloma Stage III Multiple Myeloma T-cell Large Granular Lymphocyte Leukemia Testicular Lymphoma Waldenström Macroglobulinemia 收起 << Phase 1 Phase 2 Active, not recruiting - United States, Washington ... 展开 >> Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium Seattle, Washington, United States, 98109 Italy University of Torino Torino, Italy, 10126 收起 <<
NCT01723839 Chronic Lymphocytic Leukemia (... 展开 >>CLL) 收起 << Phase 2 Active, not recruiting August 2018 United States, New Jersey ... 展开 >> John Theurer Cancer Center at HackensackUMC Hackensack, New Jersey, United States, 07601 收起 <<
NCT00544466 Leukemia Myel... 展开 >>odysplastic Syndromes 收起 << Phase 1 Phase 2 Active, not recruiting July 2019 United States, California ... 展开 >> City of Hope Medical Center Duarte, California, United States, 91010-3000 收起 <<

Fludarabine 参考文献

[1]White EL, Shaddix SC, et al. Comparison of the actions of 9-beta-D-arabinofuranosyl-2-fluoroadenine and 9-beta-D-arabinofuranosyladenine on target enzymes from mouse tumor cells. Cancer Res. 1982 Jun;42(6):2260-4.

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

[3]Tseng WC, Derse D, et al. In vitro biological activity of 9-beta-D-arabinofuranosyl-2-fluoroadenine and the biochemical actions of its triphosphate on DNA polymerases and ribonucleotide reductase from HeLa cells. Mol Pharmacol. 1982 Mar;21(2):474-7.

[4]Weiss L, Abdul-Hai A, 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.

[5]Pievani A, Michelozzi IM, et al. Fludarabine as a cost-effective adjuvant to enhance engraftment of human normal and malignant hematopoiesis in immunodeficient mice. Sci Rep. 2018 Jun 14;8(1):9125.

[6]Pharmacokinetics of fludarabine

Fludarabine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.51mL

0.70mL

0.35mL

17.53mL

3.51mL

1.75mL

35.06mL

7.01mL

3.51mL

Fludarabine 技术信息

CAS号21679-14-1
分子式C10H12FN5O4
分子量 285.232
别名 氟达拉宾 ;F-ara-A;NSC 118218;HSDB 6964;Fludarabinum
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 25 mg/mL(87.65 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

5%DMSO+40%PEG300+5%Tween80+50%water 8 mg/mL

Tags: Fludarabine | 21679-14-1 | F-ara-A | NSC 118218 | NSC118218 | NSC 118218 | NSC-118218 | DNA Synthesis Inhibitor | Cell Cycle/DNA Damage | Stem Cell/Wnt | JAK/STAT Signaling | Apoptosis | Nucleoside Antimetabolite/Analog | DNA/RNA Synthesis | STAT | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Fludarabine 纯度/质量文件 | Fludarabine 亚型比较 | Fludarabine 生物活性 | Fludarabine 细胞研究 | Fludarabine 动物研究 | Fludarabine 临床数据 | Fludarabine 参考文献 | Fludarabine 实验方案 | Fludarabine 技术信息

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