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Fludarabine Phosphate

Name: Fludarabine Phosphate
Brand: TargetMol
SKU: T6501
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6501Cas No. 75607-67-9

Alias NSC 312887 Phosphate, fludara Phosphate, F-ara-AMP, F-ara-A (NSC 312887) Phosphate

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.

Fludarabine Phosphate

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Purity: 99.78%

Catalog No. T6501Alias NSC 312887 Phosphate, fludara Phosphate, F-ara-AMP, F-ara-A (NSC 312887) PhosphateCas No. 75607-67-9

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

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.78%

Color:White

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COA HNMR LCMS

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.
Targets&IC50	DNA polymerase α:1.1 μM(Ki ), DNA polymerase δ:1.3 μM(Ki)
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)
Synonyms	NSC 312887 Phosphate, fludara Phosphate, F-ara-AMP, F-ara-A (NSC 312887) Phosphate

Chemical Properties

Molecular Weight	365.21
Formula	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
Relative Density.	2.39 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

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.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.48 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	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

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc