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Fludarabine Phosphate (Fludara)

磷酸氟达拉滨
Catalog No.
A8317
抑制STAT1激活和DNA合成
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 454.00
现货
10mg
¥ 627.00
现货
50mg
¥ 1,990.00
现货
200mg
¥ 3,818.00
现货

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A

背景

Fludarabine phosphate is a STAT-1 activation inhibitor and a DNA synthesis inhibitor. Fludarabine 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.

文献引用

化学属性

StorageStore at -20°C
M.Wt365.21
Cas No.75607-67-9
FormulaC10H13FN5O7P
SynonymsFludura
Solubilityinsoluble in EtOH; ≥17.6 mg/mL in DMSO; ≥6.7 mg/mL in H2O with gentle warming and ultrasonic
Chemical Name[(2R,3S,4S,5R)-5-(6-amino-2-fluoropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate
SDFDownload SDF
Canonical SMILESC1=NC2=C(N1C3C(C(C(O3)COP(=O)(O)O)O)O)N=C(N=C2N)F
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试验操作

Cell experiment:[1]

Cell lines

Human T lymphoblastoid cells, CCRF-CEM

Reaction Conditions

0.3 ~ 100 μM fludarabine phosphate for 5 h incubation

Applications

Fludarabine phosphate (0.3 ~ 100 μM) was dose-dependently converted to F-ara-ATP in cells. However, the incorporation of F-ara-ATP into DNA was self-limited. At 0.3 ~ 10 μM fludarabine phosphate, the amount of the F-ara-AMP incorporated into DNA increased in a dose-dependent manner, but could not further increased at fludarabine phosphate concentrations greater than 10 μM.

Animal experiment:[2]

Animal models

Mice bearing P388 leukemia

Dosage form

234 mg/kg

Injected intraperitoneally

Applications

Fludarabine phosphate administered as a single dose resulted in fewer cells surviving therapy in mice bearing P388 leukemia, accompanied by a greater percentage of increase in life span (110%) and increased median survival time.

Note

The technical data provided above is for reference only.

References:

1. Huang P, Chubb S, Plunkett W. Termination of DNA synthesis by 9-beta-D-arabinofuranosyl-2-fluoroadenine. A mechanism for cytotoxicity. Journal of Biological Chemistry, 1990, 265(27): 16617-16625.

2. Avramis VI, Plunkett W. Metabolism and therapeutic efficacy of 9-beta-D-arabinofuranosyl-2-fluoroadenine against murine leukemia P388. Cancer Research, 1982, 42(7): 2587-2591.

生物活性

Description Fludarabine is an inhibitor of STAT1 activation and a DNA synthesis.
Targets DNA synthesis          
IC50            

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