AAL-993 is a potent VEGFR inhibitor with IC50s of 130 nM, 23 nM and 18 nM for VEGFR1, VEGFR2 and VEGFR3, respectively. AAL993 has a weak inhibitory effect on other tyrosine kinases. AAL993 also shows potent antiangiogenic and antitumor activities.

VEGFR1:130 nM, VEGFR2:23 nM, VEGFR3:18 nM

AAL993 suppressed HIF-1α expression through the inhibition of ERK without affecting Akt phosphorylation[1].

AAL993 (24-100 mg/kg; p.o.) inhibited both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases in B16 melanoma xenograft model[2]. AAL993 potently inhibited VEGF-induced angiogenesis with an ED50 value of 7 mg/kg in an implant model[2].