Three protein-tyrosine kinases (VEGFR1, VEGFR2, and VEGFR3) and two non-protein kinase co-receptors (neuropilin-1 and neuropilin-2) make up the vascular endothelial growth factor (VEGF) family of receptors. The extracellular component of VEGFRs, which has seven immunoglobulin-like domains, one transmembrane domain, and a split tyrosine kinase domain, make up typical tyrosine kinase receptors (TKRs). VEGFR-1 binds to VEGF-A, -B, and PlGF; VEGFR-2 is activated by VEGF-A, -C, -D, and -E; and VEGFR-3 is particular to VEGF-C and -D. The consensus model for ligand-induced activation of RTKs states that VEGF binds to a cognate VEGFR to cause receptor dimerization, which then triggers the activation of protein kinases, autophosphorylation of tyrosine residues in the intracellular domains of the receptor, and the initiation of signaling pathways like PI3K/AKT and MAPK/ERK1/2.VEGFR signaling is tightly controlled at many different levels, including receptor expression levels, the availability and affinities of its various ligands for binding, the presence of VEGF-binding co-receptors, non-VEGF-binding auxiliary proteins, and inactivating tyrosine phosphatases, as well as the rate of receptor cellular uptake, extent of receptor degradation, and speed of recycling.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V0515 | Vatalanib (PTK-787; ZK222584; CGP79787) 2HCl | 212141-51-0 | Vatalanib (PTK787 or ZK-222584, cpg-79787 2HCl) 2HCl is a novel, potent and orally bioavailable inhibitor of VEGFR2/KDR with potential anticancer activity. |
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V81730 | VEGFR-2-IN-30 | VEGFR-2-IN-30 is a VEGFR-2 inhibitor (IC50= 66 nM). | |
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V80191 | VEGFR-2-IN-31 | VEGFR-2-IN-31 (compound 3i) is a potent VEGFR-2 inhibitor (IC50=8.93 nM) and an anti-prostate cancer agent. | |
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V80186 | VEGFR-2-IN-32 | VEGFR-2-IN-32 (Comp 3a) is an inhibitor (blocker/antagonist) of VEGFR-2 with IC50 of 8.93 nM. | |
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V79893 | VEGFR-2-IN-33 | VEGFR-2-IN-33 (Compound 4d) is a VEGFR inhibitor (IC50= 61.04 nM). | |
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V79021 | VEGFR-2-IN-35 | VEGFR-2-IN-35 (compound 7) is a potent VEGFR-2 inhibitor (antagonist) with IC50=37 nM. | |
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V81728 | VEGFR-2/AURKA-IN-1 | VEGFR-2/AURKA-IN-1 (compound 5e) is a thiazolidin-4-one analogue with anti-glioma activity (IC50= 6.43 μM, LN229). | |
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V81729 | VEGFR-2/c-Met-IN-1 | VEGFR-2/c-Met-IN-1 is a dual (bifunctional) inhibitor of VEGFR-2 and c-Met with IC50 of 138 nM and 74 nM respectively. | |
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V79271 | VEGFR2-IN-4 | VEGFR2-IN-4 (compound 25) is a potent and specific VEGFR2 kinase inhibitor (antagonist) with a GI50 value of 0.7 nM. | |
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V28284 | XL999 | 705946-27-6 | XL999, a Spectrum Selective Kinase Inhibitor(TM) (SSKIs), is a potent inhibitor of key RTKs implicated in the development and maintenance of tumor vasculature and in the proliferation of some tumor cells. |
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V0525 | ZM 306416 (CB676475) | 690206-97-4 | ZM-306416 (CB-676475)is a novel and potent tyrosine kinaseinhibitor of VEGFR1 (vascular endothelial growth factor receptor 1) with potential antineoplastic activity. |
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V0523 | ZM 323881 HCl | 193000-39-4 | ZM323881 HCl (ZM-323881 Hydrochloride) is a novel, potent and selective tyrosine kinase VEGFR2 inhibitor with potential antitumor activity. |
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