2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. VEGFR
  5. VEGFR2/KDR/Flk-1 Isoform

VEGFR2/KDR/Flk-1

VEGFR2 (KDR/Flk-1) is a receptor tyrosine kinase that serves as a central signal transducer for vascular endothelial growth factor (VEGF)-driven angiogenesis and endothelial cell development[1]. Upon binding VEGF ligands, including VEGF-A and certain processed forms of VEGF-C and VEGF-D, VEGFR2 undergoes activation and tyrosine phosphorylation, initiating downstream signaling pathways that regulate endothelial proliferation, migration, survival, and neovascularization[2]. Mechanistically, VEGFR2 signaling is essential for vascular network formation and maintenance, and it supports endothelial cell survival through anti-apoptotic signaling programs. In pathological settings, VEGFR2 plays a critical role in tumor angiogenesis and other forms of disease-associated neovascularization, making this receptor a major focus of vascular biology and translational research[1]. Compared with the related VEGF receptor isoform VEGFR1 (Flt-1), VEGFR2 functions as the principal mediator of angiogenic signaling, whereas VEGFR1 displays distinct signaling properties and can negatively regulate VEGFR2-dependent responses[2][3]. Experimental studies further demonstrate that blockade of VEGFR2, but not VEGFR1, inhibits VEGF-induced endothelial tube formation, highlighting the dominant role of VEGFR2 in angiogenic processes[4]. Consequently, VEGFR2 has become an important therapeutic and experimental target, and multiple VEGF/VEGFR2 pathway inhibitors have been developed to suppress pathological angiogenesis in cancer and other vascular disorders[1].

Cat. No. 상품명 효과 Purity
  • HY-170551
    CA IX/VEGFR-2-IN-3
    		Inhibitor
    CA IX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. CA IX/VEGFR-2-IN-3 exhibits anticancer activity, inhibiting the growth of MCF-7 breast cancer cells (with an IC50 of 22.33 μM) and mouse fibroblast cell line 3T3 (where cell viability is less than 40% at a concentration of 100 μM). CA IX/VEGFR-2-IN-3 can be used for research in the field of cancer treatment.
  • HY-178968
    VEGFR-2-IN-76
    		Inhibitor
    VEGFR-2-IN-76 (Compound GL-3) is a potent VEGFR-2 inhibitor with an IC50 value of 5.44 μM. VEGFR-2-IN-76 can be used for cancer research.
  • HY-143491
    VS 8
    		Inhibitor
    VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells).
  • HY-168073
    EGFR/VEGFR2-IN-1
    		Inhibitor
    EGFR/VEGFR2-IN-1 (Compound 10e) is a VEGFR-2 and EGFR inhibitor (IC50: 0.26 and 0.14 μM respectively). EGFR/VEGFR2-IN-1 inhibits tubulin polymerization with an IC50 of 40.9 μM. EGFR/VEGFR2-IN-1 induces apoptosis. EGFR/VEGFR2-IN-1 can be used for research of antileukemia and antilymphoma.
  • HY-144795
    VEGFR-2-IN-14
    		Inhibitor
    VEGFR-2-IN-14 (Compound 5) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-14 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis.
  • HY-106374
    Elpamotide
    		Inhibitor
    Elpamotide is an epitope peptide derived from VEGFR2. Elpamotide induces cytotoxic T lymphocytes (CTLs) to kill VEGFR2-expressing endothelial cells. Elpamotide has potential immunostimulatory and antineoplastic activities. Elpamotide can be used in the research of cancer, such as pancreatic cancer.
  • HY-163747
    VEGFR-2-IN-47
    		Inhibitor
    VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma .
  • HY-180292
    Tubulin/VEGFR-2-IN-2
    		Inhibitor
    Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma.
  • HY-146230
    VEGFR-2-IN-26
    		Inhibitor
    VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells.
  • HY-156635
    TIE-2/VEGFR-2 kinase-IN-3
    		Inhibitor
    TIE-2/VEGFR-2 kinase-IN-3, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC50 values of 6.9 nM and 3.5 nM, respectively. TIE-2/VEGFR-2 kinase-IN-3 can be used for the research of angiogenesis.
  • HY-175635
    EGFR/VEGFR2-IN-6
    		Inhibitor
    EGFR/VEGFR2-IN-6 (Compound 3k) is a dual-functional inhibitor of EGFR and VEGFR2 with IC50s of 10.53 and 3.37 μM for EGFR and VEGFR2, respectively. EGFR/VEGFR2-IN-6 has significant anti-proliferation activity against breast cancer cells, and induces G0/G1 cell cycle arrest and cell apoptosis, especially early apoptosis. EGFR/VEGFR2-IN-6 can be used for cancers research.
  • HY-149415
    Multi-kinase-IN-5
    		Inhibitor
    Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.
  • HY-182354
    VEGFR2-IN-84
    		Inhibitor
    VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors.
  • HY-156637
    TIE-2/VEGFR-2 kinase-IN-4
    		Inhibitor
    TIE-2/VEGFR-2 kinase-IN-4, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC50 values of 5.2 nM and 5.1 nM, respectively. TIE-2/VEGFR-2 kinase-IN-4 can be used for the research of angiogenesis.
  • HY-145856
    VEGFR-2-IN-11
    		Inhibitor
    VEGFR-2-IN-11 (Compound 8h) is a potent VEGFR-2 inhibitor with an IC50 of 60.27 nM. VEGFR-2-IN-11 shows antitumor activity and induces cell apoptosis.
  • HY-149630
    VEGFR2/HDAC1-IN-1
    		Inhibitor
    VEGFR2/HDAC1-IN-1 (compound 13) is a potent VEGFR-2/HDAC dual inhibitor, with IC50s of 57.83 nM and 9.82 nM, respectively. VEGFR2/HDAC1-IN-1 arrests the cell cycle at the S and G2 phases, and induces apoptosis in HeLa cells. VEGFR2/HDAC1-IN-1 exhibits anti-angiogenic effect.
  • HY-179046
    VEGFR-2-IN-78
    		Inhibitor
    VEGFR-2-IN-78 (Compound 6b) is a potent VEGFR-2 inhibitor with an IC50 of 0.21 μM. VEGFR-2-IN-78 exhibits selective cytotoxicity against A-498 and MDA-MB-231 cells. VEGFR-2-IN-78 has antioxidant activity. VEGFR-2-IN-78 can be used in anti-angiogenesis research.
  • HY-157965
    ZINC09875266
    		Inhibitor
    ZINC09875266 is a dual inhibitor targeting VEGFR2 and FAK that can be used in cancer research.
  • HY-146229
    VEGFR-2-IN-25
    		Inhibitor
    VEGFR-2-IN-25 (compound 5d) is a highly potent VEGFR-2 inhibitor with an IC50 value of 12.1 nM. VEGFR-2-IN-25 can be used for researching anticancer.
  • HY-179032
    VEGFR-2-IN-77
    		Inhibitor
    VEGFR-2-IN-77 (Compound 10) is a VEGFR-2 inhibitor with an IC50 value of 139 nM. VEGFR-2-IN-77 inhibits the PI3K/AKT/mTOR pathway. VEGFR-2-IN-77 exhibits selective cytotoxicity, being particularly sensitive to leukemia and prostate cancer cells. VEGFR-2-IN-77 causes cell cycle arrest and apoptosis, inhibiting cell migration and invasion. VEGFR-2-IN-77 can be used for the study of leukemia and prostate cancer.
Cat. No. 상품명 / Synonyms Species Source
Cat. No. 상품명 / Synonyms Application Reactivity