ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
ZK-261991 inhibits cellular receptor autophosphorylation in KDR-PAECs with an IC50 of 2 nM. ZK991 inhibits VEGFR-3 autophosphorylation concentration dependently with an IC50 of 20 nM.
ZK991 results in a significantly reduced recruitment of CD11b+ and LYVE-1+ cells into the murine cornea. ZK991 significantly improves the graft survival rate after corneal transplantation.