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
(726)
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VEGFR Agonists
(7)
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VEGFR Antagonists
(6)
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VEGFR Activators
(17)
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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
(6)
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VEGFR Ligands
(5)
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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 (823)
Related Products (823)
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Recombinant Proteins (36)
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Antibodies (9)
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VEGFR Isoform Comparison
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Sunitinib-d10
0 ImagesSynonyms: SU 11248-d10Sunitinib-d10 (SU 11248-d10) is a deuterium labeled Sunitinib. Sunitinib 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.
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Ponatinib-d8
0 ImagesSynonyms: AP24534-d8
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(Z)-FeCP-oxindole
0 Images(Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM.
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VEGFR2-IN-7
0 ImagesVEGFR2-IN-7 (compound E) is an inhibitor of VEGFR2. VEGFR2-IN-7 can used in study cancers.
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Zifibancimig
0 ImagesSynonyms: RO-7250284Zifibancimig (RO-7250284) is a monoclonal antibody against VEGF-A and Ang-2, with affinities of 4 pM and 2 pM, respectively. Zifibancimig has high stability, maintains target-binding capability under physiological stress and storage conditions, and is designed for sustained long-term ocular delivery via the Port Delivery implant device. Zifibancimig can be used in the research of retinal diseases.
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Vandetanib hydrochloride
0 ImagesCat. No.: HY-10260BCAS No.: 524722-52-9Synonyms: ZD6474 hydrochlorideVandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
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Sunitinib Malate (Standard)
0 ImagesCat. No.: HY-10255RCAS No.: 341031-54-7Synonyms: SU 11248 Malate (Standard)Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
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Midostaurin (Standard)
0 ImagesSynonyms: PKC412 (Standard); CGP 41251 (Standard)Midostaurin (Standard) is the analytical standard of Midostaurin. This product is intended for research and analytical applications. Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
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Nintedanib (Standard)
0 ImagesSynonyms: BIBF 1120 (Standard)Nintedanib (Standard) is the analytical standard of Nintedanib. This product is intended for research and analytical applications. 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.
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Sunitinib (Standard)
0 ImagesCat. No.: HY-10255ARCAS No.: 557795-19-4Synonyms: SU 11248 (Standard)Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. 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.
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Axitinib (Standard)
0 ImagesSynonyms: AG-013736 (Standard)Axitinib (Standard) is the analytical standard of Axitinib. This product is intended for research and analytical applications. 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.
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Sitravatinib malate
0 ImagesCat. No.: HY-16961ACAS No.: 2244864-88-6Synonyms: MGCD516 malate; MG-516 malateSitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
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Dovitinib lactate hydrate
0 ImagesCat. No.: HY-B0062CAS No.: 915769-50-5Synonyms: TKI258 lactate hydrate; CHIR-258 lactate hydrate
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Cabozantinib hydrochloride
0 ImagesCat. No.: HY-13016ACAS No.: 1817759-42-4Synonyms: XL184 hydrochloride; BMS-907351 hydrochlorideCabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
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Regorafenib mesylate
0 ImagesCat. No.: HY-10331BCAS No.: 835621-08-4Synonyms: BAY 73-4506 mesylateRegorafenib (BAY 73-4506) mesylate 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 mesylate shows very robust antitumor and antiangiogenic activity.
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Sorafenib-d4
0 ImagesSynonyms: Bay 43-9006-d4Sorafenib-d4 (Bay 43-9006-d4) is the deuterated-labeled Sorafenib (HY-10201). 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.
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Fursultiamine (Standard)
0 ImagesFursultiamine (Standard) is the analytical standard of Fursultiamine. This product is intended for research and analytical applications. Fursultiamine is a vitamin B1 derivative, has anti-nociceptive and antineoplastic activity. Fursultiamine can be used for vitamin B1 deficiency, osteoarthritis (OA) and cancer research.
