计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 2 篇同行评审文献引用。
概述
Fludarabine is a prodrμg converted to free nucleoside 9-β-D-arabinosyl-2-fluoroadenine (F-ara-A). F-ara-A enters cells and accumulates as 5’-triphosphate. Interferes with DNA synthesis and repair. Induces apoptosis of cancer cells and RNA transcription inhibitor.DNA synthesis and methylation inhibitor;A cell permeable agent that interferes with DNA synthesis and repair; also inhibits RNA transcription
Information
Fludarabine (NSC 118218, FaraA, Fludarabinum) is aSTAT1 activationinhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also aDNA synthesisinhibitor in vascular smooth muscle cells. Fludarabine inducesapoptosis.
In vitro
Fludarabine efficiently inhibits the proliferation of RPMI 8226 cells with IC50 of 1.54 μg/mL. The IC50 of Fludarabine against MM.1S and MM.1R cells is 13.48 μg/mL and 33.79 μg/mL, respectively. In contrast, U266 cells are resistant to Fludarabine with IC50 of 222.2 μg/mL. Fludarabine treatment results in increased number of cells in the G1 phase of cell cycle, accompanied with a concomitant reduction of cells at the S phase of cell cycle in a time-dependent manner. Fludarabine induces a cell cycle block and triggers apoptosis in MM cells. Fludarabine triggers time-dependent cleavage of caspase-8, -9, and -3, -7, followed by PARP cleavage. Fludarabine increases expression of Bax in a time-dependent fashion, while the expression of Bak doesn\'t change. After exposure to Fludarabine for 12 hours, RPMI 8226 cells shows a loss of membrane potential with 61.05% of the cells expressing low fluorescence of rhodamine 123 compared with 8.62% of cells in untreated control. To enhance solubility, Fludarabine is formulated as the monophosphate (F-ara-AMP, fudarabine), which is instantaneously and quantitatively dephosphorylated to the parent nucleoside upon intravenous infusion. Inside the cells rephosphorylation occurs which leads to fuoroadenine arabinoside triphosphate (F-ara-ATP), the major cytotoxic metabolite of F-ara-A. Fludarabine can also induce pro-inflammatory stimulation of monocytic cells, as evaluated by increased expression of ICAM-1 and IL-8 release. Fludarabine does not affect the growth of ovarian cancer cell lines, whereas it induces marked and dose-dependent inhibition of proliferation in melanoma cell lines. Fludarabine induces significant reduction of STAT-1 phosphorylation, whereas it does not change JAK2 activation. Interestingly, Fludarabine does not significantly affect the phosphorylation of these three STAT proteins. Fludarabine (1.5 mg) significantly prevents STAT-1 phosphorylation and also reduces the increased amount of this protein. No significant changes are demonstrated in JAK2 phosphorylation at 2 days, but Fludarabine inhibits JAK2-increased expression at 7 days. Fludarabine specifically inhibits STAT-1 activation without affecting other STAT proteins and consequently diminishes VSMC proliferation.
In vivo
Tumors treated with PBS grow rapidly to approx-imately 10-fold their initial volume in 25 day, whereas, the tumors in the Fludarabine at 40 mg/kg increase less than 5-fold. A significant antitumor effect of 40 mg/kg Fludarabine on RPMI8226 tumor growth is demonstrated. RPMI8226 tumors treated with 40 mg/kg Fludarabine at day 10 increase apoptotic nuclei. Fludarabine is effective in suppressing RPMI8226 myeloma xenografts in SCID mice.
Cell Data
cell lines：
Concentrations：2 μg/mL
Incubation Time：24 hours
Powder Purity:≥99%
规格
英文别名
FaraA, Fludarabinum | (2R,3S,4S,5R)-2-(6-amino-2-fluoro-9H-purin-9-yl)-5-(hydroxymethyl)-tetrahydrofuran-3,4-diol
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Fludarabine (NSC 118218)
生化机理
氟达拉滨（NSC 118218，FaraA，Fludarabinum）是一种 STAT1 激活抑制剂，可导致 STAT1 蛋白（和 mRNA）的特异性耗竭，但不会导致其他 STAT 的耗竭。也是血管平滑肌细胞的 DNA 合成抑制剂。氟达拉滨可诱导细胞凋亡。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
核糖核苷酸还原酶催化亚基 M1 抑制剂；核糖核苷酸还原酶调节亚基 M2 抑制剂
名称和识别符
EC号
244-525-5
分子类型
小分子
Isomeric SMILES
C1=NC2=C(N=C(N=C2N1[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)O)F)N
分子量
285.23
Beilstein号
1225932
Reaxy-Rn
3038524
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3038524&ln=
技术文档
高级数据
关联靶点（人）
RRM1
Tclin
核糖核苷二磷酸还原酶大亚基(Ribonucleoside-diphosphate reductase large subunit)
(1 活性数据)
RRM2
Tclin
核糖核苷二磷酸还原酶亚基M2(Ribonucleoside-diphosphate reductase subunit M2)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 43 mg/mL (197.02 mM); Ethanol: 43 mg/mL (197.02 mM); Water: Insoluble;
比旋光度
18° (C=0.1,EtOH)
熔点
260 °C
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H302: 吞食有害
预防措施声明
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P317: 如果被吞咽：请寻求医疗帮助。
WGK Germany
3
Merck Index
4126
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）