VEGFR
Vascular endothelial growth factor receptor
VEGFRs consist of three subtypes, the fms-like tyrosine kinase Flt-1 (VEGFR1/Flt-1), the kinase domain region, also referred to as fetal liver kinase (VEGFR2/KDR/Flk-1), and Flt-4 (VEGFR3). Each receptor has seven immunoglobulinlike domains in the extracellular domain, a single transmembrane region, and a consensus tyrosine kinase sequence interrupted by a kinase insert domain. VEGFR1 and 2 are expressed on vascular endothelial cells, whereas VEGFR3 is expressed on lymphatic endothelial. The VEGF family members VEGF-A, -B, -C, -D, -E, and PlGF, and the human immunodeficiency (HIV) Tat protein bind in specific patterns to three related receptor protein tyrosine kinases, VEGFR1, 2, and 3, and induce the formation of homo- and heteromeric receptor complexes. Binding of VEGF to VEGFR causes dimerization and autophosphorylation of the receptor. Intracellular proteins such as VEGFR-associated protein (VRAP), PLC, and Sck that associate with specific tyrosine residues of VEGFR are phosphorylated upon receptor activation. Several signal transduction pathways are activated by the binding of VEGF to its receptor, leading to increased proliferation, survival, permeability, and migration of cells.
VEGFR Isoform Specific Products
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VEGFR Inhibitors
(719)
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VEGFR Agonists
(7)
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VEGFR Antagonists
(6)
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VEGFR Activators
(15)
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VEGFR Modulators
(6)
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VEGFR Chemical
(1)
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VEGFR Inducer
(1)
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VEGFR Degraders
(4)
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VEGFR Ligands
(6)
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VEGFR Proteins
(36)
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VEGFR-1 Proteins
(10)
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VEGFR-3 Proteins
(7)
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VEGFR Related Products (811)
Related Products (811)
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Recombinant Proteins (36)
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Antibodies (9)
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VEGFR Isoform Comparison
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VEGFR-2-IN-89
0 ImagesCat. No.: HY-184720VEGFR-2-IN-89 is a VEGFR-2 inhibitor with an IC50 of 77 nM. VEGFR-2-IN-89 potently inhibits c-Met kinase activity with an IC50 of 0.152 μM, and also exhibits good inhibitory activity against EGFR (IC50 = 0.269 μM) and PDGFR-β kinase (IC50 = 0.301 μM). VEGFR-2-IN-89 displays anticancer activity against liver cancer. VEGFR-2-IN-89 can be used in the research of hepatocellular carcinoma.
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NPA101.3
0 ImagesCat. No.: HY-183931CAS No.: 1839155-15-5NPA101.3 is an orally active RET receptor tyrosine kinase and VEGFR2 inhibitor (RET IC50 = 0.001 μM, RETV804M IC50 = 0.008 μM, VEGFR2 IC50 = 0.003 μM). NPA101.3 inhibits purified TRKA (IC50 = 32 nM) and CSF1R (IC50 = 46 nM). NPA101.3 completely suppresses tumor formation in RET/C634Y-transformed cells and also attenuates tumor formation in HRAS/G12V-transformed cells. NPA101.3 can be used in the research of RET-driven cancers.
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EGFR/VEGFR2-IN-4
0 ImagesCat. No.: HY-10368CAS No.: 870962-74-6EGFR/VEGFR2-IN-4 (Compound 19) is the irreversible inhibitor for EGFR and VEGFR-2 with IC50 of 18.7 nM and 102.3 nM, under the presence of 1 μM ATP.
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VEGFR-2-IN-80
0 ImagesCat. No.: HY-181173VEGFR-2-IN-80 is a VEGFR-2 inhibitor with an IC50 of 2.206 μM. VEGFR-2-IN-80 interacts with ATP-binding residues of VEGFR-2 to inhibit its kinase activity. VEGFR-2-IN-80 suppresses formation of capillary-like networks, exerts cytotoxic effects against various human cancer cells, and suppresses growth of HCT116 xenografts. VEGFR-2-IN-80 can be used for the research of colorectal cancer.
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Bevasiranib sodium scrambled negative control
0 ImagesCat. No.: HY-153484CBevasiranib sodium scrambled negative control is the sequence scrambled negative control of Bevasiranib sodium.
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Multi-kinase-IN-8
0 ImagesCat. No.: HY-179439Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma.
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BI-836880
0 ImagesCat. No.: HY-P992323BI-836880 is a humanized bispecific nanobody and a selective inhibitor of VEGF and ANG2, with a Kd of 16 pM for hANG2, an EC50 of 1.4 nM for VEGF165, and an EC50 of 2.3 nM for VEGF121. BI-836880 blocks ERK phosphorylation downstream of VEGF-A as well as TIE2 phosphorylation downstream of ANG2. BI-836880 does not inhibit ANG1-mediated TIE2 phosphorylation. BI-836880 exerts anti-angiogenic effects, reduces the number of immature endothelial vessels in tumor tissues, and inhibits tumor growth in preclinical models. BI-836880 can be used in the research of pancreatic cancer, non-small cell lung cancer, renal cell carcinoma, ovarian cancer, colon cancer, and Lewis lung cancer.
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VEGFR2 AUTOTAC-1
0 ImagesCat. No.: HY-187534VEGFR2 AUTOTAC-1 is a VEGFR2 AUTOTAC degrader. VEGFR2 AUTOTAC-1 recruits p62, activates the autophagy-lysosome pathway through the p62-LC3 axis cascade, forms a ternary complex with VEGFR2 and p62, and drives UPS-independent post-translational degradation of VEGFR2. VEGFR2 AUTOTAC-1 induces G1 phase arrest and endogenous apoptosis in cells via the mitochondrial and caspase apoptotic pathways, thereby inhibiting cancer cell proliferation, migration and malignant phenotypes; meanwhile, it inhibits endothelial cell tube formation, migration and endothelial-mesenchymal transition by regulating E-cadherin and MMP2. VEGFR2 AUTOTAC-1 is applicable to research related to triple-negative breast cancer.(Pink: VEGFR2 target protein ligand (HY-187558); Blue: E3 ligase ligand (HY-W014292); Black: Linker)
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Emodic acid
0 ImagesEmodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, ERK and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells.
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GSK-3β/VEGFR2-IN-1
0 ImagesCat. No.: HY-184741GSK-3β/VEGFR2-IN-1 is an orally active dual inhibitor of GSK-3β (IC50 = 325 nM) and VEGFR2 (IC50 = 78 nM). GSK-3β/VEGFR2-IN-1 suppresses the phosphorylation of VEGFR2, AKT, MEK and ERK, inhibits human tongue squamous cell carcinoma cells migration and suppresses formation of HUVECs, exhibits low toxicity towards other cancer cells and normal cells, demonstrates significant antitumor efficacy in a CAL27 xenograft mouse model. GSK-3β/VEGFR2-IN-1 can be used for the study of tongue squamous cell carcinoma.
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VEGFR-2-IN-71
0 ImagesCat. No.: HY-175018VEGFR-2-IN-71 is a dual VEGFR2/tubulin inhibitor. VEGFR-2-IN-71 inhibits tumor cell proliferation and induces apoptosis and cell cycle arrest. VEGFR-2-IN-71 inhibits angiogenesis in the chick chorioallantoic membrane (CAM) model. VEGFR-2-IN-71 inhibits tumor growth in the HGC-27 xenograft model by inhibiting VEGFR2 and tubulin. VEGFR-2-IN-71 has low oral bioavailability in rats. VEGFR-2-IN-71 can be used in cancer research.
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Taurocholic acid-d4 sodium
0 ImagesCat. No.: HY-N0545S2Synonyms: Sodium taurocholate-d4-1 ; N-Choloyltaurine-d4-1 sodiumTaurocholic acid-d4-1 sodium (Sodium taurocholate-d4-1) is the deuterium labeled Taurocholic acid sodium (HY-N0545). Taurocholic acid sodium (Sodium taurocholate) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid sodium has immunoregulation effect.
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Multi-kinase-IN-12
0 ImagesCat. No.: HY-18692CAS No.: 597544-21-3Multi-kinase-IN-12 is a non-selective multi-target inhibitor, with IC50 values against human targets as follows: Flt3 < 0.001 μM, c-Src 0.002 μM, KDR 0.004 μM, Eph-A2, MNK-1 and Flt1 0.011 μM, Lck 0.016 μM, Rsk1 0.21 μM, and α2 subunit of AMPK 0.041 μM. Multi-kinase-IN-12 can be used in research related to solid tumors.
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R916562
0 ImagesCat. No.: HY-104075CAS No.: 1037798-41-6R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
