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AG1296
- Development stage
- Unknown
- Lead developer
- Weizmann Institute of Science
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Intraperitoneal, Subcutaneous, Intrathecal
01
Overview
AG1296 (also known as Tyrphostin AG 1296) is a potent and selective small molecule inhibitor of the Platelet-Derived Growth Factor Receptor (PDGFR) tyrosine kinase. It belongs to the tyrphostin family of compounds and acts as an ATP-competitive inhibitor, blocking the autophosphorylation of both PDGFRα and PDGFRβ isoforms. Beyond PDGFR, AG1296 also demonstrates inhibitory activity against other related receptor tyrosine kinases, including FLT3 and c-Kit. In preclinical research, AG1296 is widely used as a tool to study the role of PDGF signaling in various cancers, particularly high-grade gliomas (HGG) and glioblastomas, where it has been shown to suppress cell proliferation and inhibit the induction of oncogenic long non-coding RNAs like LINC02283. While it is a valuable research reagent for investigating signal transduction and oncogenesis, AG1296 is not currently used as a clinical therapeutic agent.
- Other names
- 6,7-Dimethoxy-2-phenylquinoxaline
02
Targets
FGFR (Fibroblast growth factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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