Efdamrofusp alfa is a bispecific fusion protein. Efdamrofusp alfa is capable of neutralizing both VEGF isoforms and C3b/C4b. Efdamrofusp alfa can be used for the research of neovascular age-related macular degeneration (nAMD) and other complement-related ocular conditions[1].
Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF。Naphazoline nitrate can be used for non-bacterial conjunctivitis research[1][2].
EGFR-IN-26 is a EGFR inhibitor extracted from patent WO2019162323A1 compound I-028. EGFR-IN-26 can be used for the research of cancer[1].
Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells[1]. Isolinderalactone suppresses the expression of B-cell lymphoma 2 (Bcl-2), survi
AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) and VEGF receptor 2 (VEGFR2) with IC50 values of 1 and 3 nM, respectively.
VEGFR-2-IN-28 (compound 12c) is a potent VEGFR-2 inhibitor with IC50 value of 0.83 µM. VEGFR-2-IN-28 induces apoptosis and has anticancer activity[1].
PTC299 is a dihydroorotate dehydrogenase (DHODH) inhibitor, has broad and potent activity against hematological cancer cells[1]. PTC299, also an orally bioavailable VEGF inhibitor, acts through posttranscriptional regulation of VEGF mRNA under conditions of cellular stress[2].
FGFR3-IN-2 (compound 18b) is a potent and selective FGFR3 inhibitor, with IC50s of 4.1 nM and 570 nM for FGFR3 and VEGFR2, respectively. FGFR3-IN-2 can be used for the research of bladder cancer[1].
Olinvacimab (TTAC-0001) is a fully human anti-VEGFR2 monoclonal antibody. Olinvacimab inhibits VEGF binds to KDR with a Kd value of 0.23 nM. Olinvacimab has antiangiogenic activity. Olinvacimab can be used for the research of recurrent glioblastoma and breast cancer[1].
Sozinibercept (OPT 302; VGX-300) is a soluble form of VEGFR-3, potently inhibits the activity of VEGF-C/D, which are the proangiogenic factors, inhibiting angiogenesis and vascular leakage. Sozinibercept also inhibits diabetic retinal edema in rats[1][2][3].
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway[1].
Pegaptanib sodium is an RNA aptamer directed against vascular endothelial growth factor (VEGF)-165. Pegaptanib could be used for the study of neovascular age-related macular degeneration (AMD) [1].
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. CBO-P11 is modified with a nearinfrared cyanine dye bearing an alkyne function, allowing both “click” coupling on azido-modified nanoparticles and fluorescence labelling[1].
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[1].
VEGFR-2-IN-27 (compound 7a) is a highly potent VEGFR-2 inhibitor with an IC50 value of 14.8 nM. VEGFR-2-IN-27 can be used for researching anticancer[1].
Abicipar pegol (AGN-150998, MP0112) is an anti-VEGF DARPin molecule, a novel class of small proteins containing ankyrin repeat domains engineered to bind with high specificity and affinity to target proteins. Abicipar pegol effectively inhibits angiogenesis and vascular permeability and is used in the study of diseases related to ocular inflammation by intravitreal injection, reducing mean retinal thickness and leakage area[1][2].
MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer[1].
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2)[1].
Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs)[1].
BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research[1].
SU5204, a tyrosine kinase inhibitor extracted from patent US5792783A, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively[1].
Hydroxytanshinone IIA is a hydroxylated metabolite of Tanshinone IIA. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2[1].
Semaxinib (SU5416) is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) with an IC50 of 1.23 μM.
Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis[1].
Ranibizumab (RG-6321) (anti-VEGF) is a humanized anti-VEGF monoclonal antibody fragment and can recognize all VEGF-A isoforms (VEGF110, VEGF121, and VEGF165)[1]. Ranibizumab (anti-VEGF) slows vision loss in vivo and is used for wet age-related macular degeneration (AMD) research[1].
c-Met-IN-11 (compound 3) is a potent c-MET and VEGFR-2 inhibitor, with IC50 values of 41.4 and 71.1 nM, respectively[1].
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis[1].
Suvemcitug is an IgG1κ antibody targeting VEGF derived from the African hare (Oryctolagus cuniculus)[1].
Tarcocimab (OG1953) is a humanized anti-VEGFA monoclonal antibody (IgG1 type). Tarcocimab is available for research in retinal vein occlusion (RVO) and wet age-related macular degeneration (AMD).