1-PHENYL-3-H-8-OXA-2,3-DIAZA-CYCLOPENTA[A]INDEN

Description

GTP 14564 is an inhibitor of class III receptor tyrosine kinases (IC₅₀s = 0.3 μM for c-Fms, c-Kit, ITD-FLT3 and 1 μM for PDGFRβ). It is without effect against a panel of non-receptor tyrosine and serine/threonine kinases. GTP 14564 blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5.

Uses

GTP 14564 is a class III receptor tyrosine kinase (RTK) inhibitor.

Definition

ChEBI: 3-phenyl-1H-benzofuro[3,2-c]pyrazole is a member of pyrazoles and a ring assembly.

Biological Activity

Potent, selective inhibitor of class III receptor tyrosine kinases (IC 50 values are 0.3 μ M for c-Fms, c-Kit, FLT3 and ITD-FLT3 and 1 μ M for PDGFR β ). Displays no selectivity for ERK1, ERK2, EGFR, MEK1, HER2, Src, Abl, PKC, PKA and Akt (IC50 > 10 μ M). Inhibits FL-dependent proliferation in BaF/ITD-FLT3 cells more potently than BaF/wt-FLT3 cells; anti-leukaemic.