GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters[1].
GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses[1].
GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo[1].
| Animal Model: | Male Balb/c mice[1] |
| Dosage: | 5 mg/kg, 20 mg/kg |
| Administration: | 5 mg/kg intravenously or 20 mg/kg orally |
| Result: | | AUC_inf (min*ug/mL) | 292.37 | | AUC_inf (hrs*nM | 11647 | | Cmax(nM) | 4386.08 | | Tmax(hrs) | 0.50 | | Clast (nM) | 636.16 | | T1/2(hrs) | 2.30 | | Vss(L/kg) | 9.18 | | F (%) | 44.82 | |
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| Animal Model: | p210 xenograft model[1] |
| Dosage: | 50 or 100 mg/kg |
| Administration: | oral, twice daily, for 7 days |
| Result: | Could normalize blood counts and spleen size. |
| Animal Model: | Bone marrow transduction/transplantation model[1] |
| Dosage: | 75 mg/kg |
| Administration: | twice daily |
| Result: | Showed no significant response (alone).
Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.
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