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Fluorocyclopentenylcytosine

Cat. No. M22390
Fluorocyclopentenylcytosine Structure
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Biological Activity

Fluorocyclopentenylcytosine

Chemical Information
Molecular Weight 257.22
Formula C10H12FN3O4
CAS Number 865838-26-2
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] Beatrice Balboni, et al. Expert Opin Investig Drugs. RX-3117 (fluorocyclopentenyl cytosine): a novel specific antimetabolite for selective cancer treatment

[2] Dzjemma Sarkisjan, et al. PLoS One. The Cytidine Analog Fluorocyclopentenylcytosine (RX-3117) Is Activated by Uridine-Cytidine Kinase 2

[3] Mi Young Yang, et al. Anticancer Res. A novel cytidine analog, RX-3117, shows potent efficacy in xenograft models, even in tumors that are resistant to gemcitabine

[4] Godefridus J Peters. Nucleosides Nucleotides Nucleic Acids. Novel developments in the use of antimetabolites

[5] Godefridus J Peters, et al. Invest New Drugs. Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360)

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