Fludarabine Phosphate (NSC 118218)

Alias: F-ara-A (NSC 312887); Phosphate; Fludara; Beneflur; 2FaraAMP; NSC312887; NSC-312887

Cat No.:V1472 Purity: ≥98%

COA Product Data Instructions for use SDS

Fludarabine Phosphate (NSC 118218) Chemical Structure CAS No.: 75607-67-9
Product category: DNA(RNA) Synthesis

This product is for research use only, not for human use. We do not sell to patients.

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Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Fludarabine phosphate (formerly F-ara-A; Fludara; Beneflur; 2FaraAMP; NSC312887; NSC-312887), the phosphate salt of Fludarabine, is an adenosine analog and potent STAT-1 activation inhibitor with potential antineoplastic activity. It suppresses the synthesis of DNA. The antiviral medication vidarabine (ara-A) is also known as fludarabine phosphate, which is the phosphate salt of fludarabine, a fluorinated nucleotide antimetabolite analog.

Biological Activity I Assay Protocols (From Reference)

Targets

DNA polymerase α ( Ki = 1.1 μM ); DNA polymerase δ ( Ki = 1.3 μM )

ln Vitro

Fludarabine phosphate dramatically lowers cell viability in a dose-dependent manner. PBS or the control vector, ACE-GFP, do not affect fludarabine phosphate at any of the tested concentrations. When ACE-PNP is exposed to for 24 hours, fludarabine phosphate, at concentrations of 2.5, 5, and 10 μg/mL, significantly reduces cell viability when compared to PBS and ACE-GFP.

ln Vivo

Fludarabine Phosphate is harmful to mice lacking tumors. When fludarabine phosphate is given as a single dose, the maximum tolerated dose (LD10) is 234 mg/kg. 375 mg/kg is the 50% lethal dose. When administered as a single dose, fludarabine phosphate causes a greater percentage of life span (110%) and increased median survival time in mice with P388 leukemia, but also reduces the number of cells surviving therapy.[3]

Cell Assay

After five hours of Fludarabine Phosphate incubation, the cells are twice cleaned in warm, drug-free medium. In Dulbecco's medium supplemented with 20% fetal bovine serum (pre-warmed to 37 °C), 800 cells are combined with 1.3 mL of 0.25% soft agar. The mixture is then incubated in a tissue culture dish for 10 days (humidified 5% CO₂, 37 °C). Under a microscope, colonies with more than 40 cells are scored at the conclusion of the incubation period. The percentage of survival above untreated control cells is used to express the cytotoxic effect of the drugs.

Animal Protocol

Mice: In nude mice (nu/nu), subcutaneous injections of parental and E. Coli PNP-expressing D54MG (human glioma) tumor cells (2×10⁷ cells) are made into the flanks. As previously mentioned, D54 tumor cells that have been stably transduced with E. coli PNP are prepared. Calipers are used to measure tumors, and the weight is estimated using the formula (length × width²)/2=mm³, which is then converted to milligrams (mg) assuming a given density. Unless otherwise indicated, eight separate injections of roughly 20 μL each are used to inject therapeutic drugs, the adenoviral vector expressing E. coli PNP (Ad/PNP), or vehicle controls into D54 tumors in 150 μL volumes in an attempt to distribute the administered agent uniformly. For every treatment group, a minimum of six mice are analyzed. Every day the mice are observed, and twice a week body weights and tumor measurements are taken. The difference in median days to two doublings (or median days to 600 mg for the D54 and DU145 (human prostate cancer) analysis) between the drug-treated and vehicle-treated groups is used to calculate T-C, or tumor growth delay. Total growth inhibition (TGI) is the evaluation point for the NIH-H322M (human non-small cell lung cancer) study due to tumor proliferation characteristics. TGI is calculated as the mean delta of the control group less the mean delta of the treated group divided by the mean delta of the control group. The change in tumor weight for each animal between day 36 and day 59 is denoted by delta. To statistically compare growth data between treatment groups, the time to the evaluation point for each animal is used as the end point for a life table analysis, a Mann-Whitney rank sum test, or a student's t-test. All significant findings are validated and replicated in comparable circumstances. When tumors weigh 250–300 mg (approximately 1.5%–1.75% of the total animal weight), treatment is started.

References

[1]. J Biol Chem . 1990 Sep 25;265(27):16617-25.

[2]. Invest New Drugs . 1984;2(3):263-5.

[3]. Cancer Res . 1982 Jul;42(7):2587-91.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C10H13FN5O7P

Molecular Weight

365.21

Exact Mass

365.05

Elemental Analysis

C, 32.89; H, 3.59; F, 5.20; N, 19.18; O, 30.67; P, 8.48

CAS #

75607-67-9

Related CAS #

21679-14-1; 75607-67-9(Fludarabine phosphate)

Appearance

White solid powder

SMILES

C1=NC2=C(N=C(N=C2N1[C@H]3[C@H]([C@@H]([C@H](O3)COP(=O)(O)O)O)O)F)N

InChi Key

GIUYCYHIANZCFB-FJFJXFQQSA-N

InChi Code

InChI=1S/C10H13FN5O7P/c11-10-14-7(12)4-8(15-10)16(2-13-4)9-6(18)5(17)3(23-9)1-22-24(19,20)21/h2-3,5-6,9,17-18H,1H2,(H2,12,14,15)(H2,19,20,21)/t3-,5-,6+,9-/m1/s1

Chemical Name

[(2R,3S,4S,5R)-5-(6-amino-2-fluoropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate

Synonyms

F-ara-A (NSC 312887); Phosphate; Fludara; Beneflur; 2FaraAMP; NSC312887; NSC-312887

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~73 mg/mL (~199.9 mM)

Water: ~2 mg/mL (~5.5 mM)

Ethanol: <1 mg/mL

Solubility (In Vivo)

30%Propylene glycol, 5%Tween 80, 65% D5W: 30 mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.7382 mL	13.6908 mL	27.3815 mL
	5 mM	0.5476 mL	2.7382 mL	5.4763 mL
	10 mM	0.2738 mL	1.3691 mL	2.7382 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

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Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01163357	Active Recruiting	Drug: bortezomib Drug: tacrolimus	Plasma Cell Leukemia Loss of Chromosome 17p	City of Hope Medical Center	January 28, 2011	Phase 1
NCT02048813	Active Recruiting	Drug: Ibrutinib Biological: Rituximab	Small Lymphocytic Lymphoma Anemia	National Cancer Institute (NCI)	February 20, 2014	Phase 3
NCT03342196	Active Recruiting	Drug: Melphalan Drug: Thiotepa	Leukemia	Case Comprehensive Cancer Center	March 21, 2018	Phase 2
NCT02250937	Active Recruiting	Drug: Busulfan Drug: Cladribine	Myelodysplastic Syndrome Acute Myeloid Leukemia	M.D. Anderson Cancer Center	October 27, 2014	Phase 2
NCT02629809	Active Recruiting	Drug: Cyclophosphamide Drug: Ibrutinib	Chronic Lymphocytic Leukemia Small Lymphocytic Lymphoma	M.D. Anderson Cancer Center	March 18, 2016	Phase 2

Biological Data