Ifebemtinib (BI 853520, IN10018) is potent, highly selective and orally active inhibitor of PTK2/FAK with IC50 of 1 nM in cell-free assays.
BI 853520 inhibits only 4 enzymes at 10 uM in a panel of 264 tyrosine and serine/threonine kinases.
BI 853520 inhibits the colony formation of PC-3 cells with EC50 of 3 nM.
BI 853520 suppresses PTK2 autophosphorylation in tissue samples from both human tumor xenografts and mouse skin.
BI 853520 demonstrates anti-tumor activity in vivo.
