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VEGFR

VEGFR

Three protein-tyrosine kinases (VEGFR1, VEGFR2, and VEGFR3) and two non-protein kinase co-receptors (neuropilin-1 and neuropilin-2) make up the vascular endothelial growth factor (VEGF) family of receptors. The extracellular component of VEGFRs, which has seven immunoglobulin-like domains, one transmembrane domain, and a split tyrosine kinase domain, make up typical tyrosine kinase receptors (TKRs). VEGFR-1 binds to VEGF-A, -B, and PlGF; VEGFR-2 is activated by VEGF-A, -C, -D, and -E; and VEGFR-3 is particular to VEGF-C and -D.The consensus model for ligand-induced activation of RTKs states that VEGF binds to a cognate VEGFR to cause receptor dimerization, which then triggers the activation of protein kinases, autophosphorylation of tyrosine residues in the intracellular domains of the receptor, and the initiation of signaling pathways like PI3K/AKT and MAPK/ERK1/2. VEGFR signaling is tightly controlled at many different levels, including receptor expression levels, the availability and affinities of its various ligands for binding, the presence of VEGF-binding co-receptors, non-VEGF-binding auxiliary proteins, and inactivating tyrosine phosphatases, as well as the rate of receptor cellular uptake, extent of receptor degradation, and speed of recycling.

VEGFR related products

Structure Cat No. Product Name CAS No. Product Description
ENMD-2076 Tartrate V69467 ENMD-2076 Tartrate 1453868-32-0 ENMD-2076 Tartrate is a multi-target kinase inhibitor that can suppress Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, and PDGFRα with IC50s of 1.86, 14, 58.2, 15.9, 92.7, and 70.8, respectively.
Eutypenes I V106026 Eutypenes I Eutypenes I (compound 9) inhibits the secretion of VEGF-A and the activation of VEGFR and its downstream Erk/Akt signaling pathway.
EVT801 V69639 EVT801 1412453-70-3 EVT801 is an orally bioactive and selective VEGFR-3 inhibitor (IC50=11 nM) with anti-tumor effects.
Foretinib phosphate V94289 Foretinib phosphate 1226999-07-0 Foretinib phosphate is a small molecule drug with high oral bioavailability and potential anti-tumor activity. It can selectively inhibit the hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), thereby potentially inhibiting tumor angiogenesis, tumor cell proliferation and metastasis.
FR 111142 V136340 FR 111142 132340-44-4 FR 111142 is an angiogenesis inhibitor (IC50 = 18.4 μM) and has anti-inflammatory activity (IC50 = 20.6 μM).
Fruquintinib-d6 V118387 Fruquintinib-d6 2978508-76-6 Fruquintinib-d6 is deuterated fruquintinib.
Girancitug V119817 Girancitug 3024821-77-7 Girancitug is a humanized IgG1κ monoclonal antibody inhibitor that targets VEGFR2/KDR/CD309.
GNQWFI V106280 GNQWFI 853995-60-5 GNQWFI is an anti-Flt1 peptide and a specific antagonist of VEGFR1.
GSK248233A V103746 GSK248233A 850665-21-3 GSK248233A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 1.03 μM and 2 nM, respectively.
GW549390X V103747 GW549390X 135307-33-4 GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.26 μM and 1.2 μM, respectively.
GW701427A V103744 GW701427A 433224-56-7 GW701427A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.12 μM and 603 nM, respectively.
GW809897X V103745 GW809897X 579515-94-9 GW809897X is a dual inhibitor of Fluc and VEGFR with IC50 of 0.58 μM and 65 nM, respectively.
hCA/VEGFR-2-IN-5 V87343 hCA/VEGFR-2-IN-5 hCA/VEGFR-2-IN-5 (compound 9) is an indole-based benzenesulfonamide and a potential dual inhibitor of cancer-related hCA IX/XII and VEGFR-2, with IC50 values of 0.38 μM, 40 and 3.2 nM for VEGFR-2, hCA IX and hCA XII, respectively.
Henatinib maleate V112061 Henatinib maleate 1239269-52-3 Genatinib maleate is an orally effective small molecule multi-kinase inhibitor.
hVEGF-IN-2 V69640 hVEGF-IN-2 186610-88-8 hVEGF-IN-2 (compound 19) is a selective VEGF (Flk-1) receptor tyrosine kinase inhibitor (antagonist) with IC50 of 2.5 μM.
hVEGF-IN-3 V101434 hVEGF-IN-3 46739-60-0 hVEGF-IN-3 (Compound 9) is a potent hVEGF inhibitor.
IMPDH2-IN-4 V93715 IMPDH2-IN-4 IMPDH2-IN-4 (compound 2d), a mycophenolic acid analog, is a selective IMPDH2 inhibitor with a Ki of 1.8 μM.
Inlecitug V137961 Inlecitug 2997627-68-4 Inlecitug is a chimeric monoclonal antibody that targets human KDR (kinase insertion domain receptor).
K-106 V115214 K-106 83647-33-0 K-106 (KPI-285) is a VEGFR antagonist that also inhibits neurotrophic tyrosine kinase receptor (NTRK).
KLTWQELYQLKYKGI V69633 KLTWQELYQLKYKGI 917760-16-8 KLTWQELYQLKYKGI (QK) is a VEGF mimetic peptide that binds to VEGF receptors and competes with VEGF.
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