GNF-5

Research use only, not for human use.

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).

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). Cell Viability Assay Cell Line:wild type and mutant Bcr-Abl expressing Ba/F3 cells Concentration:0.2, 0.8 and 1.6 μM Incubation Time:48 h Result:Inhibited wild-type Abl in a non-ATP competitive fashion.

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. Animal Model:Male Balb/c mice Dosage:5 mg/kg, 20 mg/kg Administration:5 mg/kg intravenously or 20 mg/kg orally. Animal Model:p210 xenograft modelDosage:50 or 100 mg/kgAdministration:oral, twice daily, for 7 daysResult:Could normalize blood counts and spleen size.Animal Model:Bone marrow transduction/transplantation modelDosage:75 mg/kgAdministration:twice dailyResult:Showed no significant response (alone). Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.

GNF-5 | GNF 5 | GNF5.

Tyrosine Kinase

Bcr-Abl

Bcr-Abl

Cancer

——

778277-15-9

418.37

C20H17F3N4O3

>98% (HPLC)

Ethanol: 20 mg/mL warmed (47.8 mM); DMSO: 83 mg/mL (198.38 mM)

O=C(NCCO)C1=CC=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=C1

N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide

(-20℃)

With Ice Pack

≥ 2 years