GNF-7 inhibitsBcr-Abl WT andBcr-Abl T315I with IC50 of 133 nM and 61 nM, respectively.
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The BCR-ABL oncogene is generated by the Philadelphia chromosome (Ph) translocation, fusing the BCR gene to the ABL gene. The BCR-ABL fusion protein has elevated ABL tyrosine kinase activity that is critical for transformation of hematopoietic cells[3].
GNF-7 is a multikinase inhibitor. It is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies[4].GNF-7 inhibited necroptosis in both human and mouse cells, while not protecting cells from apoptosis. Drug affinity responsive target stability assay (DARTS) demonstrated that it binds with RIPK1 and RIPK3. GNF-7 inhibited RIPK1 and RIPK3 kinase activities and thus disrupted RIPK1-RIPK3 necrosome complex formation. In vivo, GNF-7 ameliorated both cisplatin- and ischemia/reperfusion-induced AKI. Orally administration of GNF-7 attenuated renal cell necrosis and reduced pro-inflammatory responses in mouse models of AKI[5].
GNF-7 potently inhibits wild-type Bcr-Abl (IC50<5 nM) and Bcr-Abl mutants such as T315I (IC50=11 nM), G250E (IC50<5 nM), E255V (IC50=10 nM), F317L (IC50<5 nM) and M351T (IC50<5 nM) in cellular assays. GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model. GNF-7 exhibits moderate oral bioavailability (mice 36%) and Cmax (mice 3616 nM) following oral administration (mice 20 mg/kg).GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg)[6].
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