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Fludarabine Phosphate (NSC 312887 Phosphate) 是一种腺苷和脱氧腺苷类似物,与 dATP 竞争,并入到 DNA,可以抑制 DNA 聚合酶 α、核糖核苷酸还原酶和 DNA 引发酶,从而中断 DNA 合成并抑制肿瘤细胞生长。
别名 磷酸氟达拉滨, NSC 312887 Phosphate, fludara Phosphate, F-ara-AMP, F-ara-A (NSC 312887) Phosphate
Fludarabine Phosphate (NSC 312887 Phosphate) 是一种腺苷和脱氧腺苷类似物,与 dATP 竞争,并入到 DNA,可以抑制 DNA 聚合酶 α、核糖核苷酸还原酶和 DNA 引发酶,从而中断 DNA 合成并抑制肿瘤细胞生长。

| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 100 mg | ¥ 99 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 99 | 现货 |
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| 产品描述 | Fludarabine Phosphate (NSC 312887 Phosphate) is the phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase, and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth. |
| 靶点活性 | DNA polymerase δ:1.3 μM(Ki), DNA polymerase α:1.1 μM(Ki ) |
| 体外活性 | Fludarabine Phosphate的最大耐受剂量为234 mg/kg.Fludarabine对小鼠的LD50为375 mg/kg.Fludarabine Phosphate对于无肿瘤的小鼠有毒性.在携带P388白血病的小鼠中,Fludarabine Phosphate可诱导细胞存活治疗的数量减少,寿命更大比例地增加110%,平均存活时间增加. |
| 体内活性 | Fludarabine Phosphate完全抑制DNA聚合酶α/δ(Ki:1.1/1.3 μM)。在体外,DNA聚合酶δ可将Fludarabine Phosphate从结合的DNA上切除。Fludarabine Phosphate与三磷酸脱氧腺苷竞争性地结合到延伸DNA链的A位点,使DNA链延伸的终止人DNA聚合酶α比δ更能将Fludarabine Phosphate结合到DNA中。 |
| 细胞实验 | Cells are incubated with Fludarabine Phosphate for 5 hr and washed twice with drug-free warm medium. 800 cells are mixed with 1.3 mL of 0.25% soft agar in Dulbecco's medium supplemented with 20% fetal bovine serum (pre-warmed to 37 ℃) and incubated in a tissue culture dish for 10 days (humidified 5% CO2 , 37 ℃). At the end of the incubation period, colonies of more than 40 cells are scored under a microscope. The cytotoxic effect of the drugs is expressed as a percentage of survival relative to that of untreated control cells.(Only for Reference) |
| 别名 | 磷酸氟达拉滨, NSC 312887 Phosphate, fludara Phosphate, F-ara-AMP, F-ara-A (NSC 312887) Phosphate |
| 分子量 | 365.21 |
| 分子式 | C10H13FN5O7P |
| CAS No. | 75607-67-9 |
| Smiles | Nc1nc(F)nc2n(cnc12)[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]1O |
| 密度 | 2.39 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year 实际储存温度请以COA为准 | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 35 mg/mL (95.84 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: 2 mg/mL (5.48 mM), Heating is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.48 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
该溶液配制表仅适用于固体产品。对于液体产品,请根据标明的浓度或密度计算稀释方案。 | ||||||||||||||||||||||||||||||||||||
对于不同动物的给药剂量换算,您也可以参考 更多