Drug intelligence / Profile preview

UNC2025

Development stage
Preclinical
Lead developer
University of North Carolina at Chapel Hill
Modality
Small Molecules
Administration
Oral
01

Overview

UNC2025 is a potent, ATP-competitive, and orally bioavailable small molecule inhibitor of the TAM (Tyro3, AXL, MERTK) family of receptor tyrosine kinases, with high selectivity for MERTK and AXL. Developed at the University of North Carolina at Chapel Hill, it exhibits nanomolar potency against MERTK and AXL and has been shown to inhibit oncogenic signaling, induce apoptosis, and reduce colony formation in various cancer models, including acute myeloid leukemia (AML) and glioblastoma. In glioblastoma research, UNC2025 has been investigated for its ability to target both tumor cells and the immune microenvironment, specifically affecting macrophage polarization and glioblastoma stem-like cell viability. While UNC2025 is a widely used chemical probe in preclinical research, its derivative MRX-2843 is the compound that has progressed into clinical development.

02

Targets

FLT3 (Fms related receptor tyrosine kinase 3)AXL (AXL receptor tyrosine kinase)

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