Drug intelligence / Profile preview

Tie2 kinase inhibitor

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Subcutaneous, Intravitreal, Suprachoroidal, Periocular, Intraperitoneal
01

Overview

Tie2 kinase inhibitor (CAS 948557-43-5) is a potent, reversible, and selective small molecule research compound that acts as an inhibitor of the Tie2 (tunica interna endothelial cell kinase 2) receptor, also known as TEK or angiopoietin-1 receptor. It functions by targeting the ATP-binding site of the kinase with an IC50 of 250 nM, demonstrating approximately 200-fold selectivity over p38 MAPK. The compound has been studied in preclinical models for its anti-angiogenic and anti-cancer properties, showing efficacy in reducing angiogenesis in Matrigel assays and suppressing tumor growth in MOPC-315 plasmacytoma and angiosarcoma xenograft models. While it has been evaluated in a Phase I clinical trial for patients with myelodysplastic syndromes (MDS), it is primarily utilized as a research tool compound available from chemical suppliers rather than a branded pharmaceutical product.

Other names
4-(6-methoxy-2-naphthyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazoleTie2 InhibitorTie-2 InhibitorTie 2 InhibitorTie2 Kinase Inhibitor ITie-2 Kinase Inhibitor ITie 2 Kinase Inhibitor I
02

Targets

MAPK14 (p38 mitogen-activated protein kinase alpha)TEK (Tie2)

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