4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine

Biological Activity

QLT0267 is an orally active, potent and selective integrin-linked kinase (ILK) inhibitor (IC50 = 26 nM; selectivity: >1000-fold over CK2, CSK, DNA-PK, PIM1, PKB/AKT, PKC, >100-fold over ERK1, GSK3β, LCK, PKA, p70S6K, and RSK1/QLT, >10-fold over CDK1/2/5) th at inhibits ILK-dependent cellular signaling (IC50 in 2h = 1 μM against 20 nM EGF-induced pAKT Ser473 phosphorylation in Hth74 cells). QLT0267 treatment causes thyroid cancer cell cycle arrest and apoptosis, leading to anti-proliferation efficacy in cultures (IC50 <6 μM; NPA187, DRO, and K4 cell lines) and in mice in vivo (DRO xenografts-derived tumor growth; 50-100 mg/kg via daily p.o.).