1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. VEGFR

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10501A
    SU14813 maleate
    Inhibitor 99.04%
    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
    SU14813 maleate
  • HY-13302B
    CP-547632 hydrochloride
    Inhibitor 99.88%
    CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.
    CP-547632 hydrochloride
  • HY-10336
    Brivanib (alaninate)
    Inhibitor 99.45%
    Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.
    Brivanib (alaninate)
  • HY-10186
    TG 100801
    Inhibitor 98.61%
    TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
    TG 100801
  • HY-101219
    VEGFR-IN-1
    Inhibitor 98.42%
    VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively.
    VEGFR-IN-1
  • HY-132305
    VEGFR-3-IN-1
    Inhibitor 98.55%
    VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth.
    VEGFR-3-IN-1
  • HY-108868
    Mersalyl
    Inducer
    Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects.
    Mersalyl
  • HY-18309
    MET kinase-IN-4
    Inhibitor 99.46%
    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.
    MET kinase-IN-4
  • HY-19986
    AAL993
    Inhibitor 99.50%
    IC50s of 130 nM, 23 nM, and 18 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. AAL993 shows less potently inhibits other tyrosine kinases. AAL993 possesses potent antiangiogenic and antitumor properties.
    AAL993
  • HY-147133
    VEGFR2-IN-2
    Inhibitor 99.64%
    VEGFR2-IN-2 (compound 6e) is a potent and selective VEGFR2 inhibitor with an IC50 of 19.32 nM. VEGFR2-IN-2 can be used for researching
    VEGFR2-IN-2
  • HY-161025
    SYHA1813
    Inhibitor 99.46%
    SYHA1813 is a dual inhibitor of CSF1R and VEGFR. SYHA1813 has potent antitumor activity against GBM.
    SYHA1813
  • HY-P1663
    ATWLPPR Peptide
    Inhibitor 99.63%
    ATWLPPR Peptide is a biological active peptide. (This peptide is a specific VEGFR2/KDR heptapeptide antagonist, it binds VEGFR2 (KDR/flk), completely inhibiting VEGF binding to KDR and preventing VEGF-induced angiogenesis in-vivo. It specifically inhibits human endothelial cell proliferation in-vitro and totally abolishes VEGF-induced angiogenesis in-vivo.)
    ATWLPPR Peptide
  • HY-15467A
    ZM323881 hydrochloride
    Inhibitor 99.63%
    ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
    ZM323881 hydrochloride
  • HY-16018
    Ilorasertib
    Inhibitor 99.86%
    Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
    Ilorasertib
  • HY-112809
    GSK2646264
    Inhibitor 98.39%
    GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.
    GSK2646264
  • HY-10229
    Motesanib Diphosphate
    Inhibitor 99.64%
    Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
    Motesanib Diphosphate
  • HY-13785
    ZM 306416
    Inhibitor 99.80%
    ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.
    ZM 306416
  • HY-12572
    TIE-2/VEGFR-2 kinase-IN-2
    Inhibitor 99.79%
    TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research.
    TIE-2/VEGFR-2 kinase-IN-2
  • HY-N3127
    Orobol
    99.28%
    Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ).
    Orobol
  • HY-136477
    Pentagamavunon-1
    Inhibitor 99.84%
    Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
    Pentagamavunon-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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