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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V0520 | MGCD-265 analog | 875337-44-3 | MGCD-265 analog (Glesatinib analog) is a potent, orally bioavailable, and ATP-competitive multi-kinase inhibitor with potential antitumor activity. |
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V4082 | Motesanib | 453562-69-1 | Motesanib (formerly also known as AMG-706) is a novel, potent, ATP-competitive, orally bioavailable inhibitor ofVEGFR1/2/3 (vascular endothelial growth factor) with IC50 of 2 nM/3 nM/6 nM, respectively; it has potential anticancer activity; Motesanib shows similar activity against Kit, and ~10-fold more selective for VEGFR than PDGFR and Ret. |
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V0531 | Motesanib Diphosphate (AMG-706) | 857876-30-3 | Motesanib, the diphosphate salt of Motesanib (formerly AMG706) is an ATP-competitive and orally bioavailable inhibitor of vascular endothelial growth factor (VEGFR1/2/3) with potential antitumor activity. |
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V33008 | Ningetinib | 1394820-69-9 | Ningetinib, also known as CT-053, is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and<1.0 nM for c-Met, VEGFR2 and Axl, respectively. |
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V0530 | Nintedanib (Vargatef; BIBF 1120) | 656247-17-5 | Nintedanib (formerly BIBF-1120; trade name: Vargatef) is an orally bioavailable multi-kinase inhibitor with potential antineoplastic and anti-fibrotic activity. |
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V3375 | NVP-BAW2881 | 861875-60-7 | NVP-BAW2881 (also known as BAW2881) is a novel, potent and selectiveVEGFR2inhibitor with anIC50of 4 nM. |
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V0519 | Orantinib (SU 6668; NSC-702827; TSU68) | 252916-29-3 | Orantinib (formerly SU6668; TSU-68; NSC-702827; TSU 68; SU-6668) is a potent, orally bioavailable and multi-targeted receptor tyrosine kinase/RTK inhibitor with potential antineoplastic activity. |
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V0509 | OSI-930 | 728033-96-3 | OSI-930 is an orally bioavailable, potent and selective inhibitor of multi-kinase (Kit, KDR and CSF-1R) with potential antineoplastic activity. |
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V3856 | Pamufetinib (TAS-115) | 1190836-34-0 | Pamufetinib (TAS-115; TAS115) is a novel potent inhibitor of VEGFR and hepatocyte growth factor receptor (MET)-targeted kinase with anticancer activity. |
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V4131 | Pamufetinib (TAS-115) mesylate | 1688673-09-7 | Pamufetinib (TAS-115) mesylate, the mesylate salt ofPamufetinib (TAS115; TAS 115), is an inhibitor of VEGFR and c-MET with anticancer activity. |
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V0514 | Pazopanib (GW 786034; Votrient) | 444731-52-6 | Pazopanib (formerly GW-786034; GW786034; brand name Votrient) is a novel and potent multi-kinase inhibitor with potential antitumor activity. |
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V0510 | Pazopanib HCl (GW-786034; GW786034; Votrient) | 635702-64-6 | Pazopanib HCl (formerly GW786034 HCl; GW-786034; tradename Votrient) is a novel and potent multi-targetedreceptor tyrosine kinaseinhibitorwith potential anticancer activity. |
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V0513 | PD173074 | 219580-11-7 | PD173074 (PD-173074) is a novel, potent,cell permeable and selective FGFR1 inhibitor with potential antineoplastic activity. |
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V0491 | Ponatinib (AP-24534; Iclusig) | 943319-70-8 | Ponatinib (formerly known as AP24534; trade name Iclusig) is a novel, orally bioavailable multi-targeted kinase inhibitor with potent antitumor activity. |
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V2922 | R1530 | 882531-87-5 | R1530 isa small-molecule inducer of polyploidy which interferes with tubulin polymerization and mitotic checkpoint function in cancer cells, leading to abortive mitosis, endoreduplication and polyploidy. |
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V0511 | RAF265 (CHIR-265) | 927880-90-8 | RAF265 (formerly also known as CHIR265; RAF 265; RAF-265) is an orally bioavailable multi-kinase inhibitor with potential antitumor activity. |
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V0521 | SAR131675 | 1433953-83-3 | SAR131675 (SAR-131675) is a novel, potent and selective VEGFR3 inhibitor with potential antineoplastic activity. |
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V0522 | Semaxanib (SU-5416) | 204005-46-9 | Semaxanib (also known as SU5416) is a novel, potent and selective VEGFR (Flk-1/KDR) inhibitor with potential anticancer activity. |
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V2758 | Sitravatinib (MGCD-516; MG-516) | 1123837-84-2 | Sitravatinib (formerlyknown as MGCD516; MG516) is a novel and potent multi-kinase inhibitor targeting multiple RTKs (Receptor tysosine kinases) such as c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl with potential anticancer activity. |
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V0500 | SKLB1002 (SKLB-1002; SKLB 1002) | 1225451-84-2 | SKLB1002 (SKLB-1002; SKLB 1002) is a novel, potent and ATP-competitive VEGFR2 (VEGF receptor 2) inhibitor with potential antitumor activity. |
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