Molecular Formula | C20H17F3N4O3 |
Molar Mass | 418.37 |
Density | 1.385±0.06 g/cm3(Predicted) |
Boling Point | 612.4±55.0 °C(Predicted) |
Solubility | DMSO: soluble10mg/mL (clear solution) |
Appearance | powder |
Color | white to beige |
pKa | 13.36±0.46(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
In vitro study | GNF-5, when used in combination with imatinib or nilotinib, inhibits the emergence of resistance variants in vitro and exhibits additional inhibitory activity in biochemical and cellular assays against the Bcr-Abl T315I mutant. GNF-5 exhibited potent anti-proliferative activity with EC50 of 430 nM and 580 nM for wt-Bcr-Abl and E255K mutant Bcr-Abl cells, respectively. |
In vivo study | GNF-5 (100 mg/kg) showed efficacy on wild-type and T315I Bcr-Abl dependent proliferation in xenograft and bone marrow transplantation models. In addition, GNF-5 (75 mg/kg) in combination with nilotinib (50 mg/kg) increased overall survival in the T315I Bcr-Abl BMT model. |
Hazard Symbols | T - Toxic |
Risk Codes | R25 - Toxic if swallowed R36 - Irritating to the eyes |
Safety Description | S22 - Do not breathe dust. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.39 ml | 11.951 ml | 23.902 ml |
5 mM | 0.478 ml | 2.39 ml | 4.78 ml |
10 mM | 0.239 ml | 1.195 ml | 2.39 ml |
5 mM | 0.048 ml | 0.239 ml | 0.478 ml |
biological activity | GNF-5 is a selective, allosteric Bcr-Abl inhibitor with IC50 of 220 nM. |
In vitro studies | GNF-5, when used in combination with imatinib or nilotinib, it inhibits the appearance of in vitro drug resistance mutations and is resistant to Bcr-Abl T315I Mutant biochemistry and cell tests show additional inhibitory activity. GNF-5 exhibited potent antiproliferative activity with EC50 of 430 nM and 580 nM for wt-Bcr-Abl and E255K mutant Bcr-Abl cells, respectively. |
in vivo study | GNF-5 (100 mg/kg) showed efficacy on wild-type and T315I Bcr-Abl-dependent proliferation in xenograft and bone marrow transplantation models. In addition, the combination of GNF-5 (75 mg/kg) and nilotinib (50 mg/kg) can improve the total survival in the T315I Bcr-Abl BMT model. |