Fludarabine Phosphate

For research use only. Not for use in humans.

Catalog No.S1229 Synonyms: F-ara-A (NSC 312887) Phosphate

10 publications

Fludarabine Phosphate Chemical Structure

Molecular Weight(MW): 365.21

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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Selleck's Fludarabine Phosphate has been cited by 10 publications

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  • Imatinib mesylate (IM) in combination of F-AMP significantly inhibits Ki67 and c-KIT expression in GIST-T1 tumor xenografts. Tumors were collected on the day after the last treatment and were then subjected to H&E staining and immunohistochemical detection of Ki67, c-KIT, and cleaved caspase-3 expression. Representative images of H&E staining and immunohistochemical staining of Ki67, c-KIT, and cleaved caspase-3 in mice tumors. Arrows indicate the decrease in cellularity and the increase in stromal fibrosis. Magnification, x 400.

    Mol Cancer Ther 2014 13(10), 2276-87. Fludarabine Phosphate purchased from Selleck.

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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.
DNA polymerase α [1]
(Cell-free assay)
DNA polymerase δ [1]
(Cell-free assay)
1.1 μM(Ki ) 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. 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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 cells NInicW1Rem:uaX\ldoF1cW:wIHHzd4F6 MlnCOFghcA>? MnHPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjB7IN88US=> NULzfmp3OjV7NkCzNlM>
MCF7 cells MmP4VJJwdGmoZYLheIlwdiCjc4PhfS=> NHTqZWM1QCCq MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOTNizszN MXeyOVk3ODN{Mx?=
KG1 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NIPJblY1QCCq NV\DNlgxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLS|Eh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMUWg{txO NYnGfIhlOjV7NkCzNlM>
Raji cells M2HkTXBzd2yrZnXyZZRqd25iYYPzZZk> MVq0PEBp MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKjanmgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPCEQvF2= NFzNPHMzPTl4MEOyNy=>
K562 cells NHfCVYNRem:uaX\ldoF1cW:wIHHzd4F6 MmDUOFghcA>? NWO5N3JQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkSg{txO NHj0NFUzPTl4MEOyNy=>
ZR-75-1 cells NFrNWI5Rem:uaX\ldoF1cW:wIHHzd4F6 MY[0PEBp MkjNRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCcUj23OU0yKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLk[g{txO MorvNlU6PjB|MkO=
MOLT3 cells NVH5OJhOWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFTpT2I1QCCq NX7xXHFpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD65OUDPxE1? MUKyOVk3ODN{Mx?=
M-HeLa cells MnzGVJJwdGmoZYLheIlwdiCjc4PhfS=> MlTwOFghcA>? MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE1vSHXMZUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OiEQvF2= NVjaTWhbOjV7NkCzNlM>
SK-UT-1B cells MlvuVJJwdGmoZYLheIlwdiCjc4PhfS=> NVnISmVVPDhiaB?= MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLWXUMVFDKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD14IN88US=> M{\TZlI2QTZyM{Kz

... Click to View More Cell Line Experimental Data

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]


Cell Research:[1]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[3]
- Collapse
  • Animal Models: Murine Leukemia P3881
  • Formulation: Heating and subsequently injecting as cooled, supersaturated water solution.
  • Dosages: 234 mg/kg
  • Administration: A single dose i.p. at day 1
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (199.88 mM)
Water 2 mg/mL warmed (5.47 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 365.21


CAS No. 75607-67-9
Storage powder
in solvent
Synonyms F-ara-A (NSC 312887) Phosphate
Smiles NC1=NC(=NC2=C1N=C[N]2C3OC(CO[P](O)(O)=O)C(O)C3O)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04106310 Not yet recruiting Device: High-flux dialyzer|Device: Theranova dialyzer End Stage Renal Failure on Dialysis The University of Hong Kong|Baxter Healthcare Corporation December 1 2019 Phase 4
NCT03878953 Not yet recruiting Drug: rhPTH(1-84) Chronic Hypoparathyroidism Shire October 30 2019 Phase 3
NCT03943537 Not yet recruiting Drug: Intranasal Insulin Psychosis|Schizophrenia|Schizo Affective Disorder|Bipolar I Disorder Mclean Hospital October 2019 Phase 2
NCT04118842 Not yet recruiting Drug: Savolitinib|Drug: Rifampicin Solid Tumors AstraZeneca October 7 2019 Phase 1
NCT04121910 Not yet recruiting Drug: Savolitinib|Drug: Itraconazole Solid Tumour AstraZeneca|Parexel October 31 2019 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID