Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret.

Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.

Nintedanib (BIBF 1120) 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.

Nintedanib (BIBF 1120) 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.

NVP-ACC789 is an inhibitor of VEGFR-2 (FLK-1/KDR).

NVP-BAW2881 is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor

Pazopanib Hcl (GW-786034) is a novel 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.

Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-α/β, and c-Kit.

Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

Regorafenib (BAY 73-4506, Fluoro-Sorafenib) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

SAR131675 is a potent and selective VEGFR-3 inhibitor.

Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR.

SKLB1002 is a novel and potent VEGFR-2 inhibitor with an IC50 value of 32 nM.

SKLB610, a novel multi-targeted inhibitor, inhibits angiogenesis-related tyrosine kinase VEGFR2, FGFR2 and PDGFR at rate of 97%, 65% and 55%, respectively, at concentration of 10 μM in biochemical kinase assays.

SU 5205 is a VEGFR2 inhibitor.

SU-10994 is a novel VEGFR inhibitor.

SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3).

SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1with an IC50 of value of 700 nM.

SU4312(NSC86429) is a selective, cell-permeable inhibitor of VEGFR2 and PDGFR tyrosine kinases (IC50s = 0.8 and 19.4 μM, respectively).

Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

Takeda-6d has potent inhibitory activity in both B-RAF with an IC50 of 7.0 nM and VEGFR2 with an IC50 of 2.2 nM.

TAS-115 mesylate is a potent VEGFR and c-Met/HGFR kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.