Cabozantinib (formerly known as XL-184 or BMS-907351; trade name Cometriq) is a novel, orally bioavailable and potent VEGFR2 inhibitor with anticancer activity.

Ningetinib,also known as CT-053, is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and<1.0 nM for c-Met, VEGFR2 and Axl, respectively.

Motesanib (formerly also known as AMG-706) is a novel, potent, ATP-competitive, orally bioavailable inhibitor of VEGFR1/2/3 (vascular endothelial growth factor) with IC50 of 2 nM/3 nM/6 nM, respectively; it has potential anticancer activity; Motesanib shows similar activity against Kit, and ~10-fold more selective for VEGFR than PDGFR and Ret.

RAF265 (formerly also known as CHIR265; RAF 265; RAF-265) is an orally bioavailable multi-kinase inhibitor with potential antitumor activity.

SU-5408, formerly known as VEGFR2 Kinase Inhibitor I, is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase (IC50 = 70 nM).

Pazopanib (formerly GW-786034; GW786034; brand name Votrient) is a novel and potent multi-kinase inhibitor with potential antitumor activity.

SAR131675 (SAR-131675) is a novel, potent and selective VEGFR3 inhibitor with potential antineoplastic activity.

MAZ-51 is a novel, potent and selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase.

Golvatinib (formerly E-7050) is an orally bioavailable dual c-Met and VEGFR-2 inhibitor with potential antineoplastic activity.

Telatinib (formerly BAY57-9352) is an orally bioavailable multi-kinase (e.g. VEGFR, PDGFR) inhibitor with potential antineoplastic activity.