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Fludarabine Phosphate

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Purity:99.25%

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COA HNMR HPLC

Fludarabine Phosphate

Catalog No. T6501Cas No. 75607-67-9

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.

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Pack Size	Price	Availability
5 mg	$32	In Stock
10 mg	$52	In Stock
25 mg	$84	In Stock
50 mg	$117	In Stock
100 mg	$143	In Stock
200 mg	$201	In Stock
500 mg	$336	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock

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Product Introduction

Bioactivity

Description	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.
In vitro	The maximum tolerable dose of Fludarabine Phosphate is determined to be 234 mg/kg, with its LD50 (lethal dose 50%) for mice being 375 mg/kg. Notably, Fludarabine Phosphate exhibits toxicity in tumor-free mice. However, in mice carrying P388 leukemia, treatment with Fludarabine Phosphate leads to a reduction in the number of surviving cells geared towards therapy, significantly enhancing the lifespan by 110% and increasing the average survival time.
In vivo	Fludarabine Phosphate effectively inhibits DNA polymerase α/δ (Ki: 1.1/1.3 μM), demonstrating potent inhibitory activity in vitro. It is capable of being excised from bound DNA by DNA polymerase δ. Competitively binding with deoxyadenosine triphosphate at the A site for DNA chain elongation, Fludarabine Phosphate leads to the termination of DNA strand extension. Notably, human DNA polymerase α is more adept at incorporating Fludarabine Phosphate into DNA than polymerase δ.
Cell Research	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)
Alias	NSC 312887 Phosphate, fludara Phosphate, F-ara-A (NSC 312887) Phosphate, F-ara-AMP

Chemical Properties

Molecular Weight	365.21
Formula	C10H13FN5O7P
Cas No.	75607-67-9

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 35 mg/mL (95.84 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 2 mg/mL (5.47 mM)

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	2.7382 mL	13.6908 mL	27.3815 mL	136.9075 mL
5 mM	0.5476 mL	2.7382 mL	5.4763 mL	27.3815 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.2738 mL	1.3691 mL	2.7382 mL	13.6908 mL
20 mM	0.1369 mL	0.6845 mL	1.3691 mL	6.8454 mL
50 mM	0.0548 mL	0.2738 mL	0.5476 mL	2.7382 mL
100 mM	0.0274 mL	0.1369 mL	0.2738 mL	1.3691 mL

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