Fludarabine Phosphate

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

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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Cited by 10 Publications

1 Customer Review

  • 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.
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

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 NXXU[XI1WHKxbHnm[ZJifGmxbjDhd5NigQ>? NEjH[JY1QCCq MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODlizszN MnXDNlU6PjB|MkO=
MCF7 cells MkPMVJJwdGmoZYLheIlwdiCjc4PhfS=> M2\1UlQ5KGh? NILnTIVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMUOg{txO M4nMSFI2QTZyM{Kz
KG1 cells M3[2cXBzd2yrZnXyZZRqd25iYYPzZZk> MYK0PEBp NFnI[5dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvHNUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5zNTFOwG0> NYroW5o4OjV7NkCzNlM>
Raji cells NImzeIpRem:uaX\ldoF1cW:wIHHzd4F6 MnzLOFghcA>? MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKjanmgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPCEQvF2= MkG2NlU6PjB|MkO=
K562 cells NYXGbFh4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NVLlV5F6PDhiaB?= MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPCEQvF2= NFrzUGQzPTl4MEOyNy=>
ZR-75-1 cells NFjyRlhRem:uaX\ldoF1cW:wIHHzd4F6 M1\WRVQ5KGh? MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFqULUe1MVEh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwNjFOwG0> M4nUblI2QTZyM{Kz
MOLT3 cells NIS4U2lRem:uaX\ldoF1cW:wIHHzd4F6 MXK0PEBp NEHnZ4tCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUHQ{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkm1JO69VQ>? NHvNVYMzPTl4MEOyNy=>
M-HeLa cells NGXi[5BRem:uaX\ldoF1cW:wIHHzd4F6 MVq0PEBp NGTSV2FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF2tTIVN[SClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MjFOwG0> MWWyOVk3ODN{Mx?=
SK-UT-1B cells MkLWVJJwdGmoZYLheIlwdiCjc4PhfS=> MYS0PEBp NUHOfVd7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1WXC1zQjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OkDPxE1? MnXmNlU6PjB|MkO=

... 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]

Protocol

Cell Research:[1]
+ Expand
  • 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]
+ Expand
  • 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
Formula

C10H13FN5O7P

CAS No. 75607-67-9
Storage powder
in solvent
Synonyms F-ara-A (NSC 312887) Phosphate

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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