Drug intelligence / Profile preview

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

FLT3 (Fms related receptor tyrosine kinase 3)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)FGFR (Fibroblast growth factor receptor)PDGFRB (Platelet-derived growth factor receptor beta)

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