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GNF-5

(CAS No:778277-15-9)
GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.
CAS No:778277-15-9
Molecular Weight(MW):418.37
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 778277-15-9
Molecular formula(MF) C20H17F3N4O3
Molecular Weight(MW): 418.37
Alias
Solubility
In vitro DMSO 83 mg/mL (198.38 mM)
Ethanol 20 mg/mL warmed (47.8 mM)
Water <1 mg/mL
In vivo
Biological Activity
Description GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.
Targets
Bcr-Abl [1]
220 nM
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]

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]