(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.

JNJ-38158471(KDR) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50=40nM. It also inhibits closely related tyrosine kinases, Ret (180nM) and Kit (500nM). It has no significant activity (>1 microM) against VEGFR-1 and VEGF

SU-10994 is a novel VEGFR inhibitor.

Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.

ZM323881 a receptor tyrosine kinase inhibitor of VEGFR-2 (Flk-1), PDGFR-beta, EGFR, and FGFR1

ZM 323881 hydrochloride is a potent and selective inhibitor of human Flk-1 (vascular endothelial growth factor receptor 2, VEGFR-2/KDR) activity.

MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2.