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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V2879 | SKLB610 | 1125780-41-7 | SKLB610 is a novel multi-targeted kinase inhibitor with more potent inhibition of VEGFR2. |
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V15373 | SU 5205 | 3476-86-6 | SU5205 is an inhibitor (blocker/antagonist) of VEGFR2 (FLK-1) with IC50 of 9.6 μM. |
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V15375 | SU 5214 | 186611-04-1 | SU5214 is a potent VEGFR2 inhibitor (antagonist) with IC50s of 14.8 µM (FLK-1) and 36.7 µM (EGFR). |
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V15393 | SU-1498 | 168835-82-3 | SU 1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM). |
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V15399 | SU-5408 | 15966-93-5 | SU-5408, formerly known as VEGFR2 Kinase Inhibitor I, is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase (IC50 = 70 nM) |
|
V2331 | SU5204 | 186611-11-0 | SU5204 is a tyrosine kinase inhibitor (TKI) (antagonist) with IC50 of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively. |
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V2501 | SU5208 | 62540-08-3 | SU5208 inhibits vascular endothelial growth factor receptor 2 (VEGFR2). |
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V0495 | SU5402 (SU-5402; SU 5402) | 215543-92-3 | SU5402 (SU-5402; SU 5402) is a multi-targeted RTK (receptor tyrosine kinase) inhibitor with potential antineoplastic activity. |
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V15401 | SU5614 | 1055412-47-9 | SU5614 is a potent and selective FLT3 inhibitor. |
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V0497 | Sunitinib free base (SU-11248) | 557795-19-4 | Sunitinib (formerly also known as SU11248; trade name: Sutent) is a potent, orally bioavailable and multi-targeted RTK (receptor tyrosine kinase) inhibitor with potential antitumor activity. |
|
V0489 | Sunitinib Malate (SU-11248 Malate) | 341031-54-7 | Sunitinib Malate (formerly also known as SU11248 Malate; trade nameSutent)) is a potent, orally bioavailable and multi-targeted RTK (receptor tyrosine kinase) inhibitor with potent anticancer activities. |
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V81493 | T-1-MCPAB | T-1-MCPAB is a VEGFR-2 inhibitor (IC50=0.135 µM) that can effectively inhibit the migration of MCF7. | |
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V1986 | Tanshinone IIA (Dan Shen ketone) | 568-72-9 | Tanshinone IIA (Tan IIA;Dan Shen ketone),derived from phenanthrene-quinone, which is isolated from Salvia miltiorrhiza BUNGE. |
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V0532 | Telatinib (BAY 57-9352) | 332012-40-5 | Telatinib (formerly BAY57-9352) is an orally bioavailable multi-kinase (e. |
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V80000 | Telatinib mesylate (Bay 57-9352 mesylate) | 332013-26-0 | Telatinib mesylate (also known as Bay 57-9352 mesylate) is a potent and orally bioactiveVEGFR2,VEGFR3,PDGFα, andc-Kitinhibitor with potential anticancer activity. |
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V5007 | TG 100801 | 867331-82-6 | TG 100801 (TG-100801; TG100801) is an ester prodrug of TG-100572 (TG 100572). |
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V0505 | Tivozanib (AV951; KRN-951) | 475108-18-0 | Tivozanib (formerly KRN951 or AV-951; brand name Fotivda) is a novel, orally bioavailable,potent and selective inhibitor ofVEGFR(vascular endothelial growth factor receptors)with potential antineoplastic activity. |
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V27845 | UNC0064-12 | 1430089-64-7 | VEGFR-2-IN-5 is a VEGFR2 inhibitor. |
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V0494 | Vandetanib (ZD-6474) | 443913-73-3 | Vandetanib (formerly also known as ZD6474; trade name Caprelsa) is a highly potent, orally bioavailable, and selective inhibitor of VEGFR2 with potential anticancer activity. |
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V7978 | Vatalanib (PTK-787; ZK-222584; CGP-79787) | 212141-54-3 | Vatalanib ((PTK787 or ZK 222584, cpg-79787)is a novel, potent and orally bioavailable inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, it isless potent against VEGFR1/Flt-1, and is 18-fold against VEGFR3/Flt-4. |
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