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5-Fluoro-2′-deoxycytidine

Cat. No. M7804
5-Fluoro-2′-deoxycytidine Structure
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Biological Activity

5-Fluoro-2′-deoxycytidine is a mechanism based DNMT (DNA cytosine-5 methyltransferase) inhibitor, that forms a covalent link with the cysteine residue in the active site of DNMT.

Chemical Information
Molecular Weight 245.21
Formula C9H12FN3O4
CAS Number 10356-76-0
Solubility (25°C) DMSO: ≥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] Geraldine O 'Sullivan Coyne, et al. Intravenous 5-fluoro-2'-deoxycytidine administered with tetrahydrouridine increases the proportion of p16-expressing circulating tumor cells in patients with advanced solid tumors

[2] Andrei Solodinin, et al. 5-Fluoro-2'-deoxycytidine as a Probe for the Study of B/Z-DNA Transition by 19 F NMR Spectroscopy

[3] Hung-Man Yu, et al. Evaluation of 5-[ 18 F]fluoro-2'-deoxycytidine as a tumor imaging agent: A comparison of [ 18 F]FdUrd, [ 18 F]FLT and [ 18 F]FDG

[4] Marie Morfouace, et al. Preclinical studies of 5-fluoro-2'-deoxycytidine and tetrahydrouridine in pediatric brain tumors

[5] Duoli Guo, et al. Stability of 5-fluoro-2'-deoxycytidine and tetrahydrouridine in combination

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Keywords: 5-Fluoro-2′-deoxycytidine supplier, inhibitors, activators


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