Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Fludarabine Phosphate For research use only.

Fludarabine Phosphate

Synonyms: F-ara-A Phosphate, NSC 118218 Phosphate

Fludarabine Phosphate is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

Fludarabine Phosphate Chemical Structure

Fludarabine Phosphate Chemical Structure

CAS No. 75607-67-9

Purity & Quality Control

Fludarabine Phosphate Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 cells Proliferation assay 48 h Antiproliferative activity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.09 μM 25960323
MCF7 cells Proliferation assay 48 h Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.13 μM 25960323
KG1 cells Proliferation assay 48 h Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.15 μM 25960323
Raji cells Proliferation assay 48 h Antiproliferative activity against human Raji cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.4 μM 25960323
K562 cells Proliferation assay 48 h Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.4 μM 25960323
ZR-75-1 cells Proliferation assay 48 h Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.6 μM 25960323
MOLT3 cells Proliferation assay 48 h Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.95 μM 25960323
M-HeLa cells Proliferation assay 48 h Antiproliferative activity against human M-HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2 μM 25960323
SK-UT-1B cells Proliferation assay 48 h Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM 25960323
Click to View More Cell Line Experimental Data

Biological Activity

Description Fludarabine Phosphate is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
Targets
DNA polymerase α [1]
(Cell-free assay)		 DNA polymerase δ [1]
(Cell-free assay)
1.1 μM(Ki ) 1.3 μM(Ki)
In vitro
In vitro Fludarabine Phosphate is converted to F-ara-ATP in cells and then incorporated into DNA in a self-limiting manner. Fludarabine Phosphate competes with dATP for incorporation into the A site of the extending DNA strand, which results in termination of DNA strand elongation. Human DNA polymerase α incorporates more Fludarabine Phosphate into DNA than polymerase δ. Fludarabine Phosphate completively inhibits DNA polymerase α and DNA polymerase δ with Ki of 1.1 μM and 1.3 μM, respectively. DNA polymerase δ is also able to excise the incorporated Fludarabine Phosphate from DNA in vitro. [1]
Cell Research Cell lines Human T lymphoblastoid cells
Concentrations 30 μM
Incubation Time 5 hours
Method 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.
In Vivo
In vivo Fludarabine Phosphate is toxic for tumor-free mice. The maximum tolerated dose (LD10) Fludarabine Phosphate administered as a single dose is 234 mg/kg. The 50% lethal dose is 375 mg/kg. Fludarabine Phosphate administered as a single dose induces fewer number of cells surviving therapy in mice bearing P388 leukemia, accompanied by greater percentage of increase in life span (110%) and increased median survival time. [3]
Animal Research Animal Models Murine Leukemia P3881
Dosages 234 mg/kg
Administration A single dose i.p. at day 1
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05039892 Not yet recruiting
CholangiocarcinomaAdult
3D Medicines (Beijing) Co. Ltd.|3D Medicines
 December 2024 Phase 2
NCT06377293 Not yet recruiting
End-Stage Kidney Disease
Far Eastern Memorial Hospital
 November 2024 Not Applicable
NCT06398002 Not yet recruiting
Secondary Hyperparathyroidism|End-stage Kidney Disease
Iain Bressendorff|Herlev Hospital
 August 1 2024 Phase 2
NCT06383403 Not yet recruiting
Primary Biliary Cholangitis
Ipsen
 July 1 2024 Phase 3
NCT06302439 Not yet recruiting
Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 Deficiency|ATP-Binding Cassette Subfamily C Member 6 Deficiency
Inozyme Pharma|GACI Global
 May 2024 --

Chemical Information & Solubility

Molecular Weight 365.21 Formula

C10H13FN5O7P
CAS No. 75607-67-9 SDF Download Fludarabine Phosphate SDF
Smiles C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)COP(=O)(O)O)O)O)F)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (199.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 3 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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