Fludarabine Phosphate

For research use only.

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

41 publications

Fludarabine Phosphate Chemical Structure

CAS No. 75607-67-9

Fludarabine Phosphate (F-ara-A, NSC 312887) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

Selleck's Fludarabine Phosphate has been cited by 41 publications

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Biological Activity

Description Fludarabine Phosphate (F-ara-A, NSC 312887) 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 NVfpS|NuWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3z5N|Q5KGh? NX;rdW17SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkC5JO69VQ>? NYPrPGt{OjV7NkCzNlM>
MCF7 cells NWewb5lwWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1npR|Q5KGh? NVi4RYllSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkGzJO69VQ>? M33rN|I2QTZyM{Kz
KG1 cells M33LZXBzd2yrZnXyZZRqd25iYYPzZZk> MnuwOFghcA>? M1KzU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1exJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF3IN88US=> MoTsNlU6PjB|MkO=
Raji cells M3L5OHBzd2yrZnXyZZRqd25iYYPzZZk> Mn61OFghcA>? NXP1V2VySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSZYpqKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkSg{txO MWCyOVk3ODN{Mx?=
K562 cells MnHmVJJwdGmoZYLheIlwdiCjc4PhfS=> NY\DRlRxPDhiaB?= Mki1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjRizszN M2rRNFI2QTZyM{Kz
ZR-75-1 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 M4rrVVQ5KGh? M1;ibGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iWmKtO|UuOSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD62JO69VQ>? MVqyOVk3ODN{Mx?=
MOLT3 cells M2fVS3Bzd2yrZnXyZZRqd25iYYPzZZk> M360cFQ5KGh? MnT2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC57NTFOwG0> MWiyOVk3ODN{Mx?=
M-HeLa cells MoTSVJJwdGmoZYLheIlwdiCjc4PhfS=> MVi0PEBp MoD6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPLVjlUIEh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTJizszN M4rob|I2QTZyM{Kz
SK-UT-1B cells NGCyTpdRem:uaX\ldoF1cW:wIHHzd4F6 NGfES|A1QCCq NF[5OYZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMXVVNTGEIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME22JO69VQ>? NXPVOFY2OjV7NkCzNlM>

... 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]
- 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
  • 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

* 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
Smiles C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)COP(=O)(O)O)O)O)F)N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03878953 Not yet recruiting Drug: rhPTH(1-84) Chronic Hypoparathyroidism Shire|Takeda March 31 2022 Phase 3
NCT04763499 Not yet recruiting Other: freeze dried strawberry powder Vascular Dilation University of California Davis October 1 2021 Not Applicable
NCT04485039 Not yet recruiting Drug: TPOXX Smallpox SIGA Technologies|Biomedical Advanced Research and Development Authority|PPD September 15 2021 Phase 4
NCT04657146 Not yet recruiting Other: Biorepository Glioblastoma Duke University September 1 2021 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID