QLT-0267

Biological Activity

QLT0267 is an inhibitor of integrin-linked kinase (ILK; IC50 = 26 nM).1 It is greater than 10-fold selective for ILK over cyclin-dependent kinase 1 (Cdk1), Cdk2, and Cdk5, as well as greater than 1,000-fold selective for ILK over C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2), at 10 mg/ml. QLT0267 inhibits the growth of NPA187 papillary thyroid cancer cells (IC50 = ~3 μM) and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo, QLT0267 (100 mg/kg) reduces tumor growth in a DRO mouse xenograft model. It also reduces tumor volume and intratumoral blood vessel mass in a U87MG glioblastoma mouse xenograft model.2

References

1.Younes, M.N., Kim, S., Yigitbasi, O.G., et al.Integrin-linked kinase is a potential therapeutic target for anaplastic thyroid cancerMol. Cancer. Ther.4(8)1146-1156(2005) 2.Edwards, L.A., Woo, J., Huxham, L.A., et al.Suppression of VEGF secretion and changes in glioblastoma multiforme microenvironment by inhibition of integrin-linked kinase (ILK)Mol. Cancer Ther.7(1)59-70(2008)