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Fludarabine Phosphate 75607-67-9

Product Description

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Molecular Weight:

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.

Biological Activity

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.


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.

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Product Categories : DNA Damage > DNA/RNA Synthesis Inhibitor