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Fludarabine Phosphate

Catalog No. T6501 CAS 75607-67-9

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

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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Fludarabine Phosphate Chemical Structure

Fludarabine Phosphate, CAS 75607-67-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 32.00
10 mg	In stock	$ 52.00
25 mg	In stock	$ 84.00
50 mg	In stock	$ 117.00
100 mg	In stock	$ 143.00
200 mg	In stock	$ 201.00
500 mg	In stock	$ 336.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.25%

Purity: 98.26%

Biological Description

Chemical Properties

Storage & Solubility Information

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-A (NSC 312887) Phosphate, F-ara-AMP
Molecular Weight	365.21
Formula	C10H13FN5O7P
CAS No.	75607-67-9

Storage

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

Solubility Information

DMSO: 68 mg/mL (186.2 mM)

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

H2O: 2 mg/mL (5.47 mM), Heating is recommended.

References and Literature

1. Huang P, et al, J Biol Chem, 1990, 265(27), 16617-16625. 2. Umbach GE, et al. Invest New Drugs, 1984, 2(3), 263-265. 3. Avramis VI, et al. Cancer Res, 1982, 42(7), 2587-2591.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Hematonosis Compound Library Anti-Aging Compound Library Bioactive Compound Library NO PAINS Compound Library

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Keywords

Fludarabine Phosphate 75607-67-9 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis Nucleoside Antimetabolite/Analog NSC 118218 Inhibitor NSC-312887 Phosphate NSC 312887 Phosphate NSC312887 Phosphate Fludarabine fludara Phosphate inhibit F-ara-A (NSC 312887) Phosphate NSC118218 F-ara-AMP NSC-118218 inhibitor

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