gnf-5

**GNF-5** is a selective, small molecule, allosteric inhibitor of the Bcr-Abl tyrosine kinase. It is an analogue of GNF-2, distinguished by a N-hydroxyethyl carboxamide modification at the 4-position, which imparts superior pharmacokinetic properties such as increased bioavailability and a longer half-life. GNF-5 inhibits Bcr-Abl kinase by binding to the myristate-binding site and acts as a non-ATP competitive inhibitor, making it effective against both wild-type and imatinib-resistant Bcr-Abl mutants, including T315I. It induces apoptosis and cell cycle arrest in a variety of cancer cell lines (notably in CML and hepatocellular carcinoma models) by downregulating the S-phase kinase-associated protein 2 (Skp2) and upregulating tumor suppressors p27 and p21. The principal developer is Beijing Novartis Pharma, and the drug remains in preclinical development with no clinical trial results or market approvals as of 2025.

Brand names

gnf-5gnf5gnf 5

Other names

bcr-abl inhibitor III gnf-5N-(2-hydroxyethyl)-3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide