Drug Class Detail

Drug Class VEGFR2 Inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
SU11652 FGFR1 Inhibitor 21 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 VEGFR2 Inhibitor 34 SU11652 is an inhibitor of multiple tyrosine kinase receptors including Pdgfr-beta, Kdr (Vegfr2), Fgfr1, and Kit, which blocks pathway activation, promotes cell cycle arrest, and induces apoptosis of tumor cells (PMID: 12091352, PMID: 23216927).
Semaxanib SU5416 FLT3 Inhibitor 48 VEGFR1 Inhibitor 4 VEGFR2 Inhibitor 34 Semaxanib (SU5416) is an inhibitor of FLT1 (VEGFR1), KDR (VEGFR2), and FLT3, which inhibits tumor vascularization and growth (PMID: 9892193, PMID: 12351406).
Sunitinib Sutent SU011248 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 VEGFR2 Inhibitor 34 Sutent (sunitinib) inhibits KDR (VEGFR2), PDGFR, c-KIT, FLT3, RET, and CSF1R, thereby inhibiting angiogenesis and cell proliferation (NCI Drug Dictionary; PMID: 25085632). Sutent (sunitinib) is approved for neuroendocrine tumors of the pancreas, advanced renal cell carcinoma, and GIST (FDA.gov).
Foretinib GSK1363089G|XL880|EXEL-2880 MET Inhibitor 50 ROS1 Inhibitor 14 TrkA Receptor Inhibitor 7 VEGFR2 Inhibitor 34 Foretinib (GSK1363089) is a multi-kinase inhibitor with activity against several receptor tyrosine kinases, including MET, KDR (VEGFR2), as well as ROS1 and NTRK fusions, which may result in decreased tumor angiogenesis and growth (PMID: 19808973, PMID: 26372962, PMID: 29463555).
XL999 FGFR1 Inhibitor 21 FGFR3 Inhibitor 12 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 SRC Inhibitor 26 VEGFR2 Inhibitor 34 XL999 inhibits multiple tyrosine kinases including VEGFR2/KDR, FGFR1/3, PDGFR-beta, FLT3, RET, KIT, and SRC, which can result in anti-tumor activity (J Clin Oncol, 25:18s, 2007 (suppl;abstr 3591), PMID: 19581523).
Golvatinib E7050 EPHB4 Inhibitor 6 MET Inhibitor 50 VEGFR2 Inhibitor 34 Golvatinib (E7050) is a dual kinase inhibitor of c-Met and KDR (VEGFR2), which inhibits cell growth and proliferation (PMID: 25458359).
CLM3 EGFR Inhibitor (Pan) 38 RET Inhibitor 36 VEGFR2 Inhibitor 34 CLM3 is an small molecule multi-kinase inhibitor with activity against several kinases including Ret, Vegfr2, and Egfr, which potentially leads to decreased tumor cell growth (PMID: 21459081, PMID: 24423321).
SKLB646 BRAF Inhibitor 18 CRAF Inhibitor 10 SRC Inhibitor 26 VEGFR2 Inhibitor 34 SKLB646 is a multi-kinase inhibitor with activity against Src, Kdr (Vegfr2), Braf and Craf, resulting in decreased downstream signaling and potentially leading to reduced tumor growth (PMID: 26721945).
RXDX-105 AC013773|CEP-32496 ABL Inhibitor (pan) 8 ABL1 Inhibitor 4 BCR-ABL Inhibitor 23 BRAF Inhibitor 18 CRAF Inhibitor 10 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 VEGFR2 Inhibitor 34 RXDX-105 (CEP-32496) inhibits wild-type BRAF, BRAF V600E, c-RAF, ABL1 (and BCR-ABL), c-KIT, RET, PDGFR beta, and VEGFR2, potentially resulting in decreased tumor growth (PMID: 22319199).
ENMD-2076 Aurka Inhibitors 23 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FLT3 Inhibitor 48 RET Inhibitor 36 VEGFR2 Inhibitor 34 ENMD-2076 has selective inhibitory activity against Aurora kinase A and FLT3, with reduced potency against RET, KDR (VEGFR2), FGFR1, and FGFR2, preventing angiogenesis and decreasing cell proliferation (PMID: 21177375, PMID: 22921155).
Telatinib BAY 57-9352 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 VEGFR2 Inhibitor 34 VEGFR3 Inhibitor 5 BAY 57-9352 (Telatinib) inhibits VEGFR2, VEGFR3, PDGFR-beta, and KIT, which may result in decreased proliferation and angiogenesis in tumors expressing these factors (NCI Drug Dictionary).
XL647 KD019|Tesevatinib EGFR Inhibitor (Pan) 38 EPHB4 Inhibitor 6 HER2 Inhibitor 20 VEGFR2 Inhibitor 34 VEGFR3 Inhibitor 5 XL647 is an inhibitor of multiple receptor tyrosine kinases, including ERBB2 (HER2), EGFR, VEGFR2 and VEGFR3, and EphB4, potentially resulting in decreased tumor growth and angiogenesis (PMID: 17575237).
Brivanib BMS-540215 FGFR1 Inhibitor 21 VEGFR1 Inhibitor 4 VEGFR2 Inhibitor 34 Brivanib (BMS-540215) selectively binds and inhibits KDR (VEGFR2), while demonstrating moderate activity against VEGFR1 and FGFR1, which inhibits tumor angiogenesis, tumor cell growth, and induces tumor regression (PMID: 18829493, PMID: 16570908).
R916562 AXL Inhibitor 24 VEGFR2 Inhibitor 34 R916562 is a small molecule that inhibits both Axl and Vegfr2, therefore results in synergistic inhibition of tumor angiogenesis and metastasis (PMID: 28711351).
Ningetinib CT053PTSA AXL Inhibitor 24 MET Inhibitor 50 VEGFR2 Inhibitor 34 Ningetinib inhibits cMet, Vegfr2, and Axl, which may synergistically inhibits tumor cell growth (Cancer Res 2014;74(19 Suppl):Abstract nr 1755).
Apatinib Rivoceranib YN968D1 KIT Inhibitor 48 RET Inhibitor 36 SRC Inhibitor 26 VEGFR2 Inhibitor 34 Apatinib (YN968D1) is an inhibitor of receptor tyrosine kinases, including KDR (VEGFR2), RET, c-KIT, Src, and PDGFRa, which may result in reduced cell proliferation and inhibition of tumor growth (PMID: 21443688).
rebastinib DCC-2036 BCR-ABL Inhibitor 23 FLT3 Inhibitor 48 TIE2 Inhibitor 1 VEGFR2 Inhibitor 34 Rebastinib (DCC-2036) inhibits the Bcr-Abl fusion and to a lesser extent, the receptor tyrosine kinases TIE-2, FLT3, and VEGFR2 (PMID: 21481795).
PD173074 FGFR1 Inhibitor 21 FGFR3 Inhibitor 12 FGFR4 Inhibitor 7 VEGFR2 Inhibitor 34 PD173074 is an ATP-competitive inhibitor of FGFR1, FGFR3, FGFR4, and KDR (VEGFR2), which may reduce proliferation and induce apoptosis in cancer cells (PMID: 9774334, PMID: 24126887, PMID: 14715624).
TAS-115 MET Inhibitor 50 VEGFR2 Inhibitor 34 TAS-115 is a small molecule inhibitor of MET and KDR (VEGFR2), which may lead to angiogenesis blockade and tumor regression (PMID: 24140932).
PP-121 ABL Inhibitor (pan) 8 mTOR Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 VEGFR2 Inhibitor 34 PP-121 inhibits several types of kinases including, PDGFR, Hck, mTOR, KDR (VEGFR2), Src and Abl to prevent cell proliferation (PMID: 24867098).
Regorafenib Stivarga BAY 73-4506 BRAF Inhibitor 18 CRAF Inhibitor 10 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 RET Inhibitor 36 VEGFR Inhibitor (Pan) 29 VEGFR2 Inhibitor 34 Stivarga (regorafenib) is an inhibitor of several kinases including VEGFR, RET, KIT, PDGFR and RAF, thereby inhibiting tumor angiogenesis and tumor cell proliferation (PMID: 24756792). Stivarga (regorafenib) is FDA approved for colorectal cancer, hepatocellular carcinoma, and GIST (FDA.gov).
TY-011 Aurka Inhibitors 23 Aurkb Inhibitors 17 VEGFR2 Inhibitor 34 TY-011 inhibits Aurora kinase A and B, as well as KDR (VEGFR2), resulting in inhibition growth and angiogenesis in tumors (PMID: 27887633).
Sorafenib Nexavar BAY 43-9006 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RAF Inhibitor (Pan) 17 RET Inhibitor 36 VEGFR2 Inhibitor 34 Nexavar (sorafenib) is a multikinase inhibitor with activity against several kinases, including RAF kinases, VEGFR2, VEGFR3, PDGFR-beta, KIT, FLT3, RET, and CSF1R, potentially resulting in decreased tumor growth (PMID: 18445656, PMID: 15466206, PMID: 21517818). Nexavar (sorafenib) is approved for metastatic differentiated thyroid carcinoma, hepatocellular carcinoma, and renal cell carcinoma (FDA.gov).
Midostaurin Rydapt PKC412|CGP 41251 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PKC alpha Inhibitor 6 PKC beta Inhibitor 6 PKC Inhibitor (Pan) 9 VEGFR2 Inhibitor 34 Rydapt (midostaurin) is a multi-kinase inhibitor with activity against FLT3, KIT, PDGFRB, KDR (VEGFR2) and PKC, with higher selectivity for conventional PKC isoforms, which induces cell cycle arrest and apoptosis (PMID: 12124173, PMID: 23127174, PMID: 15914319). Rydapt (midostaurin) is FDA approved for FLT3-mutant AML in combination with chemotherapy, and is approved for use in aggressive systemic mastocytosis, systemic mastocytosis with associated hematological neoplasm, or mast cell leukemia as a single therapy (FDA.gov).
Cabozantinib Cometriq Cabometyx|Cabozantinib-s-malate|XL184 AXL Inhibitor 24 FLT3 Inhibitor 48 KIT Inhibitor 48 MET Inhibitor 50 RET Inhibitor 36 ROS1 Inhibitor 14 VEGFR2 Inhibitor 34 Cometriq (Cabometyx, cabozantinib) inhibits several receptor tyrosine kinases, including VEGFR2, FLT3, AXL, MET, RET, ROS1 fusions, and c-KIT (PMID: 27370605, PMID: 21926191). Cometriq (cabozantinib) is FDA approved for medullary thyroid cancer and Cabometyx (cabozantinib) is FDA approved for advanced renal cell carcinoma and in sorafenib previously treated hepatocellular carcinoma (FDA.gov).
OSI-930 KIT Inhibitor 48 VEGFR2 Inhibitor 34 OSI-930 binds and inhibits Kdr (Vegfr2) and Kit reducing cell proliferation and tumor growth (PMID: 16424037).
Anlotinib AL3818|AL-3818 VEGFR2 Inhibitor 34 VEGFR3 Inhibitor 5 Anlotinib (AL-3818) inhibits KDR (VEGFR2) and VEGFR3, thereby preventing angiogenesis and tumor cell growth (NCI Drug Dictionary).
Pz-1 RET Inhibitor 36 VEGFR2 Inhibitor 34 Pz-1 is an inhibitor with activity against Ret and Kdr, which may result in tumor growth inhibition (PMID: 26126987).
RAF265 BRAF Inhibitor 18 CRAF Inhibitor 10 VEGFR2 Inhibitor 34 RAF265 inhibits the activities of several intracellular kinases, including BRAF(V600E), BRAF(wild type), c-RAF (RAF1), VEGF receptor 2 (VEGFR2/KDR), platelet-derived growth factor receptor (PDGFR), colony-stimulating factor (CSF)1R, RET and c-KIT, SRC, STE20, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death (PMID: 22351689; NCI Drug Dictionary).
Famitinib SHR1020 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RET Inhibitor 36 VEGFR2 Inhibitor 34 VEGFR3 Inhibitor 5 Famitinib is an analog of Sutent (sunitinib), a receptor tyrosine kinase (RTK) inhibitor, which inhibits receptor tyrosine kinases including c-Kit, VEGFR2/3, PDGFR-beta, RET, and FLT3 to reduce cell proliferation and tumor growth (PMID: 23126373).
Orantinib SU6668|TSU-68 FGFR1 Inhibitor 21 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 VEGFR2 Inhibitor 34 Orantinib (SU6668) inhibits several receptor tyrosine kinases KDR, PDGFRB, FGFR1, and KIT, thereby resulting in tumor growth inhibition (PMID: 17367541, PMID: 16144927).
JI-101 EPHB4 Inhibitor 6 PDGFR-beta Inhibitor 13 VEGFR2 Inhibitor 34 JI-101 inhibits KDR (VEGFR2), PDGFR-beta, and EphB4, resulting in anti-tumor activity (PMID: 26365907).
Cediranib AZD-2171|Recentin KIT Inhibitor 48 VEGFR1 Inhibitor 4 VEGFR2 Inhibitor 34 VEGFR3 Inhibitor 5 Cediranib (AZD-2171) is an ATP-competitive inhibitor of all three vascular endothelial growth factor receptors (FLT1, KDR, and FLT4) and KIT, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth (PMID: 15899831, PMID: 24714778).
YLL545 VEGFR2 Inhibitor 34 YLL545 inhibits KDR (VEGFR2), resulting in decreased downstream signaling and potentially leading to decreased angiogenesis and reduced tumor cell proliferation and tumor growth (PMID: 27203384).
Molecular Profile Protein Effect Treatment Approaches
KDR A1065T gain of function - predicted VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL N131fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL inact mut loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Q132fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL L116fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S80R loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL C162W loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R167W loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL G114R loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL H110Q unknown mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S68fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Y112H loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Q96* loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL H115Q loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R167Q loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S111N loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R82P loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R161P loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL F148fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL N78S loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL V155fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL C77* loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
KDR Q472H gain of function VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R79P loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL P86H loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S80I loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL C162F loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S111R loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Y98H loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S68* loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL W88* loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL L184P loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL V130F loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL V74G loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL H115R loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S65W loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL R161G loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S183L loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL D126N loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL P154L loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
KDR act mut gain of function VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL P81S loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL N90I loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL W117C loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL V62fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL loss loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL S65L loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL L158P loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
KDR D717V unknown VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL L158fs loss of function - predicted mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor
VHL Y98N loss of function mTORC1 Inhibitor VEGFR Inhibitor (Pan) VEGFR2 Inhibitor