Drug intelligence / Profile preview

UNC2025A

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

Overview

UNC2025A is a potent, orally bioavailable dual inhibitor of the receptor tyrosine kinases **MERTK** (Mer tyrosine kinase) and **FLT3** (Fms-like tyrosine kinase 3). Developed at the University of North Carolina at Chapel Hill, it was designed as part of a program to target the TAM (Tyro3, Axl, Mer) family of kinases, which are frequently overexpressed in various cancers and contribute to tumor cell survival, proliferation, and immune evasion. UNC2025A exhibits high selectivity for MERTK and FLT3 over other TAM family members like AXL. In preclinical models of acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC), UNC2025A has demonstrated the ability to inhibit downstream signaling pathways, including STAT, AKT, and ERK, leading to decreased colony formation and the induction of apoptosis. It is widely utilized as a chemical probe in oncology research to elucidate the roles of MERTK and FLT3 in leukemogenesis and solid tumor progression.

02

Targets

FLT3 (Fms related receptor tyrosine kinase 3)

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