Potent and selective breast tumor kinase (Brk) inhibitor (IC50 = 30 nM). Exhibits >650-fold selectively for Brk over Aurora B kinase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also active in vivo and orally bioavailable.
Zeng et al (2011) Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. Bioorg.Med.Chem.Lett 21 5870 PMID:21855335 |Ito et al (2016) PTK6 inhibition suppresses metastases of triple-negative breast cancer via SNAIL-dependent E-cadherin regulation. Cancer Res. 76 4406 PMID:27302163