 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 778277-15-9 |
| Molecular formula(MF) | C20H17F3N4O3 |
| Molecular Weight(MW): | 418.37 |
| Alias |
| In vitro | DMSO | 83 mg/mL (198.38 mM) |
|---|---|---|
| Ethanol | 20 mg/mL warmed (47.8 mM) | |
| Water | <1 mg/mL | |
| In vivo |
| Description | GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM. | ||
|---|---|---|---|
| Targets |
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| In vitro |
GNF-5, when used in combination with imatinib or nilotinib, suppresses the emergence of resistance mutations in vitro, and displays additive inhibitory activity in biochemical and cellular assays against Bcr-Abl T315I mutant. [1] GNF-5 shows potent antiproliferative activity with EC50 of 430 nM and 580 nM against wt-Bcr-Abl and E255K mutant Bcr-Abl transformed cells, respectively. [2] |
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| In vivo | GNF-5 (100 mg/kg ) displays efficacy on wild-type and T315I Bcr-Abl dependent proliferation in xenograft and bone marrow transplantation models. Moreover, a combination of GNF-5 (75 mg/kg) with nilotinib (50 mg/kg) results in improved overall survival in a T315I Bcr-Abl BMT model. [1] |