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2'-Fluoro-2'-Deoxyadenosine is efficiently cleaved to the toxic 2-fluoroadenine (FAde) by Escherichia coli purine nucleoside phosphorylase (PNP). 2'-Fluoro-2'-Deoxyadenosine showed good in vivo activity against tumors expressing E. coli PNP. 2'-Fluoro-2'-Deoxyadenosine can be used to synthesize 2'-deoxy-2'-fluoromodified oligonucleotides that can hybridize to RNA.