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Fludarabine (NSC 118218) Phosphate DNA Synthesis/STAT1 Inhibitor

Cat.No.S1229

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

Batch: Purity: 99.91%
99.91

Cell Culture, Treatment & Working Concentration

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
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
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
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
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
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
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
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
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
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Solubility

In vitro
Batch:

DMSO : 73 mg/mL (199.88 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 3 mg/mL

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 365.21 Formula

C10H13FN5O7P

Storage (From the date of receipt)
CAS No. 75607-67-9 Download SDF Storage of Stock Solutions

Synonyms F-ara-A Phosphate, NSC 118218 Phosphate SMILES C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)COP(=O)(O)O)O)O)F)N

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
DNA polymerase α
(Cell-free assay)
1.1 μM(Ki )
DNA polymerase δ
(Cell-free assay)
1.3 μM(Ki)
In vitro
Fludarabine Phosphate is converted to F-ara-ATP in cells and then incorporated into DNA in a self-limiting manner. This compound 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 of this chemical into DNA than polymerase δ. It 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.
In vivo
Fludarabine Phosphate is toxic for tumor-free mice. The maximum tolerated dose (LD10) of this compound administered as a single dose is 234 mg/kg. The 50% lethal dose is 375 mg/kg. This chemical 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-24)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07055477 RECRUITING
Relapsed and/or Refractory Mature T Cell Malignancy; Peripheral T-Cell Lymphoma; Angioimmunoblastic T-cell Lymphoma; Anaplastic Large Cell Lymphoma; Hepatosplenic T-cell Lymphoma; Monomorphic Epithelialtropic Intestinal Lymphoma; Enteropathy Associated T-cell Lymphoma; Cutaneous T-Cell Lymphoma; Mycosis Fungoides; Subacute Panniculitis-like T-cell Lymphoma
National Cancer Institute (NCI)
2025-09-29 PHASE1
NCT06191887 RECRUITING
B-Cell Non-Hodgkin Lymphoma; Recurrent Chronic Lymphocytic Leukemia; Recurrent Diffuse Large B-Cell Lymphoma; Recurrent Follicular Lymphoma; Recurrent Mantle Cell Lymphoma; Recurrent Marginal Zone Lymphoma; Recurrent Small Lymphocytic Lymphoma; Recurrent Transformed Chronic Lymphocytic Leukemia; Refractory Chronic Lymphocytic Leukemia; Refractory Diffuse Large B-Cell Lymphoma; Refractory Follicular Lymphoma; Refractory Mantle Cell Lymphoma; Refractory Marginal Zone Lymphoma; Refractory Small Lymphocytic Lymphoma; Refractory Transformed Chronic Lymphocytic Leukemia
Mayo Clinic
2024-03-18 PHASE1
NCT04877613 ACTIVE_NOT_RECRUITING
Metastatic Medullary Thyroid Cancer; Recurrent Thyroid Gland Medullary Carcinoma
University of Pennsylvania
2021-08-19 PHASE1
NCT03935893 ACTIVE_NOT_RECRUITING
Gastric Cancer; Colorectal Cancer; Pancreatic Cancer; Sarcoma; Mesothelioma; Neuroendocrine Tumors; Squamous Cell Cancer; Merkel Cell Carcinoma; Mismatch Repair Deficiency; Microsatellite Instability
Udai Kammula
2019-12-03 PHASE2
NCT06885697 RECRUITING
Mesothelioma; Neoplasms; Stomach Neoplasms; Pancreatic Neoplasms; Ovarian Neoplasms; Lung Neoplasms; Thymus Neoplasms; Colonic Neoplasms
National Cancer Institute (NCI)
2025-07-08 PHASE1
NCT05617625 SUSPENDED
Myelodysplastic Syndromes; Graft Vs Host Disease; Graft-versus-host-disease
Guenther Koehne
2026-06 PHASE2

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