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. Product Name Effect Purity
  • HY-10201
    Sorafenib
    		Inhibitor 99.85%
    Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
  • HY-10981
    Lenvatinib
    		Inhibitor 99.75%
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-50904
    Nintedanib
    		Inhibitor 99.94%
    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-10255A
    Sunitinib
    		Inhibitor 99.04%
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-10374
    Semaxinib
    		Inhibitor 99.92%
    Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC50 of 1.23 μM.
  • HY-10255C
    Sunitinib glucuronate
    		Inhibitor
    Sunitinib (SU 11248) glucuronate is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib glucuronate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-184142
    EYE1118
    		Inhibitor
    EYE1118 is an orally active, photoactivatable VEGFR2 inhibitor without acute hepatotoxicity. EYE1118 mediates light-enhanced inhibition via azide-functionalized receptor binding, and can utilize light-guided targeting to regulate its biodistribution in vivo. EYE1118 effectively inhibits angiogenesis, endothelial cell migration, VEGF-induced retinal leakage, and the size of choroidal neovascular lesions. EYE1118 has been applied in studies related to age-related macular degeneration, diabetic retinopathy, and choroidal neovascularization.
  • HY-111277
    CEP-14513
    		Inhibitor
    CEP-14513 is an ALK inhibitor with an IC50 of 4 nM. CEP-14513 also inhibits insulin receptor, VEGFR2, TIE2 and DLK kinases, but does not inhibit MET, IKKβ, or CDK1/2/5. CEP-14513 induces cancer cell apoptosis. CEP-14513 is applicable to research related to non-small cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroblastic tumor, and diffuse large B-cell lymphoma.
  • HY-10331
    Regorafenib
    		Inhibitor 99.93%
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
  • HY-13016
    Cabozantinib
    		Inhibitor 99.97%
    Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
  • HY-12047
    Ponatinib
    		Inhibitor 99.67%
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-10065
    Axitinib
    		Inhibitor 99.94%
    Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
  • HY-10321
    PD173074
    		Inhibitor 99.86%
    PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.
  • HY-10208
    Pazopanib
    		Inhibitor 99.91%
    Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
  • HY-10407
    SU 5402
    		Inhibitor 99.78%
    SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
  • HY-11106
    Nintedanib esylate
    		Inhibitor 99.96%
    Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-10981A
    Lenvatinib mesylate
    		Inhibitor 99.91%
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-19912
    Fruquintinib
    		Inhibitor 99.98%
    Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.
  • HY-12686
    5Z-7-Oxozeaenol
    		Inhibitor 99.60%
    5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
  • HY-10260
    Vandetanib
    		Inhibitor 99.85%
    Vandetanib (D6474) is a potent, orally active, and blood-brain-barrier penetrate inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity