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Alovudine

Cat. No. M20702
Alovudine Structure
Synonym:

CL 184824, FddThd, FLT, MIV-310

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Biological Activity

3'-Fluoro-3'-deoxythymidine (Alovudine) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer.

Chemical Information
Molecular Weight 244.22
Formula C10H13FN2O4
CAS Number 25526-93-6
Solubility (25°C) DMSO 49 mg/mL
Water 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Dana Yehudai, et al. Haematologica. The thymidine dideoxynucleoside analog, alovudine, inhibits the mitochondrial DNA polymerase γ, impairs oxidative phosphorylation and promotes monocytic differentiation in acute myeloid leukemia

[2] Lai-Ming Yung, et al. Circ Cardiovasc Imaging. Room With a View

[3] Karin Lindn, et al. Pharmacol Toxicol. Effect of probenecid and quinidine on the transport of alovudine (3'-fluorothymidine) to the rat brain studied by microdialysis

[4] Stefano Rusconi. Curr Opin Investig Drugs. Alovudine Medivir

[5] L Stahle, et al. Life Sci. Transport of alovudine (3'-fluorothymidine) into the brain and the cerebrospinal fluid of the rat, studied by microdialysis

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Keywords: Alovudine, CL 184824, FddThd, FLT, MIV-310 supplier, Reverse Transcriptase, inhibitors, activators


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