In Vitro: GNF-5 has inhibition of wild-type Abl with an IC50 value of 0.22 µM but no inhibition for myristate site mutant E505K (IC50 >10 µM).
In Vivo: GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters. GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses. GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo.