Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Foretinib is less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and with little activity to FGFR1 and EGFR.

Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.

Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM.

Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13/4.2/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

Pazopanib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.

Cediranib is a multiple RTKs inhibitor with IC50 values of <0.001μM, 0.005μM, ≤0.003μM, 0.002μM and 0.005μM for VEGFR-2, VEGFR-1, VEGFR-3, c-Kit and PDGFR-β(measured kinase activity), respectively.

Dovitinib is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM.

Linifanib is a potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively.

Vatalanib 2HCl is inhibitor of VEGFR2 or KDR with IC50 of 37 nM.

Tivozanib is an inhibitor of VEGFR1, VEGFR2 and VEGFR3 with IC50s of 30 nM, 6.5 nM, 15 nM, respectively. It can also inhibit PDGFR and c-Kit.

Lenvatinib is a multi-target inhibitor, mostly for VEGFR2 (KDR)/VEGFR3 (Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold selective for VEGFR2/3 against FGFR1, PDGFRα/β.

MGCD-265, an ATP-competitive inhibitor, can inhibit c-Met and VEGFR1, 2, 3 with IC50s of 1 nM and 3 nM, 3 nM, 4 nM, respectively. It also exhibits inhibition of Ron and Tie2.

ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.

Telatinib is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.

SAR131675 is selective inhibitor of VEGFR3 with IC50 and Ki of 23 nM, 12 nM, respectively.

Sitravatinib is an inhibitor of receptor tyrosine kinase (RTK) involved in driving sarcoma cell growth, is developed for the treatment of cancer.

BAW2881 is an inhibitor of vascular endothelial growth factor (VEGF) with IC50s of 1.0 nM-4.3 nM against VEGFR1, 2, 3 and also inhibits PDGFRβ, c-Kit, and RET.

Motesanib diphosphate is ATP-competitive inhibitor of VEGFR1, VEGFR2 and VEGFR3 with IC50 of 2 nM, 3 nM and 6 nM, respectively. It also shows better inhibitory activity against c-Kit, PDGFR, and RET.