Drug intelligence / Profile preview

HG-7-92-01

Development stage
Preclinical
Lead developer
University of Pittsburgh
Modality
Small Molecules
01

Overview

HG-7-92-01 is a potent, small-molecule pyrrolopyridine kinase inhibitor that targets the c-Fes (Fes) protein-tyrosine kinase and the FMS-like tyrosine kinase 3 (Flt3), particularly the internal tandem duplication (ITD) mutant form. It was identified as a research tool to explore the role of Fes in oncogenic signaling downstream of Flt3-ITD in acute myelogenous leukemia (AML). HG-7-92-01 demonstrates dual inhibitory activity, blocking both Fes and Flt3-ITD kinase activity in vitro and in cell-based models, leading to growth arrest and apoptosis in Flt3-ITD+ AML cell lines and patient-derived samples. While highly effective in preclinical models, it is primarily used as a chemical probe and has not yet transitioned into clinical development by a pharmaceutical sponsor.

Other names
CAS 1315355-93-1CAS1315355-93-1CAS-1315355-93-1
02

Targets

TAK1 (Transforming growth factor beta–activated kinase 1)GCK (Glucokinase)FES (Proto-oncogene tyrosine-protein kinase Fes)FLT3-ITD (Fms-like tyrosine kinase 3 with internal tandem duplication)

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