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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V0507 | Dovitinib (TKI-258, CHIR-258) | 405169-16-6 | Dovitinib (formerly TKI258 and CHIR258) is a potent, orally bioavailable and multi-targeted RTK (receptor tyrosine kinase) inhibitor with potential anticancer activity. |
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V0498 | Dovitinib (TKI258; CHIR-258 ) Lactate | 915769-50-5 | Dovitinib Lactate (formerly TKI-258 lactate; CHIR-258 lactate), abenzimidazole-quinolinone analog, is a potent, orally bioavailable andmultitargeted RTK inhibitor with potential antineoplastic activity. |
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V0516 | Dovitinib Dilactic Acid (TKI258; CHIR258) | 852433-84-2 | Dovitinib (formerly also known as TKI-258 or CHIR-258) is a potent, orally bioavailable andmulti-targeted RTK (receptor tyrosine kinase) inhibitor with potential antineoplastic activity. |
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V0528 | ENMD-2076 Tartrate | 1291074-87-7 | ENMD-2076Tartrate, the tartrate salt ofENMD-981693 (MKC-1693), is a novel, potent andorally bioactive multi-kinase inhibitorwith potential antineoplastic activity. |
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V0493 | Foretinib (GSK-1363089; XL-880; EXEL2880; GSK-089) | 849217-64-7 | Foretinib (also known as GSK1363089; XL880; EXEL-2880; GSK089) is a novel, potent, ATP-competitive small-molecule inhibitor of multipletyrosine kinases (e. |
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V3719 | Fruquintinib | 1194506-26-7 | Fruquintinib (formerly known as HMPL-013; Elunate) is a novel, potent, selective and oral small molecule inhibitor of VEGFR1/2/3 family (IC50s = 33, 0.35, and 35 nM) with strong potency and high selectivity. |
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V0524 | Golvatinib (E7050) | 928037-13-2 | Golvatinib (formerly E-7050) is an orally bioavailable dual c-Met and VEGFR-2 inhibitor with potential antineoplastic activity. |
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V79199 | hCA/VEGFR-2-IN-2 | hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual (bifunctional) inhibitor of cancer-associated hCA IX/XII and VEGFR-2. | |
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V79040 | hCA/VEGFR-2-IN-3 | hCA/VEGFR-2-IN-3 (compound 8j) is an indolinylbenzenesulfonamide and a potential dual (bifunctional) inhibitor of cancer-associated hCA IX/XII and VEGFR-2. | |
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V79440 | hCA/VEGFR-2-IN-4 | hCA/VEGFR-2-IN-4 (compound 15b) is an indolinonylbenzenesulfonamide and a potential dual (bifunctional) inhibitor of cancer-associated hCA IX/XII and VEGFR-2. | |
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V32431 | hVEGF-IN-1 | 1637443-98-1 | hVEGF-IN-1, a quinazoline analogue, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilizes the G-quadruplex structure. |
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V2149 | JK-P3 | 942655-44-9 | JK-P3 is novel inhibitor of VEGFR-2. JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50 = 7.8 μM). |
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V0502 | Ki8751 | 228559-41-9 | Ki8751 (Ki-8751), aquinolyloxyphenyl-urea analog,is a novel,cell-permeableand selective inhibitor of VEGFR2 (Flk-1)with potential anticancer activity. |
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V0527 | KRN 633 | 286370-15-8 | KRN 633 (KRN-633) is a novel, potent, selective, cell-permeable, reversible,and ATP-competitive inhibitor of VEGFR1/2/3 with potential antitumor activity. |
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V0508 | Lenvatinib (E7080; ER-203492-00) | 417716-92-8 | Lenvatinib (formerly E-7080, ER-203492-00; tradename Lenvima among others) is a potent and orally bioavailablemulti-targeted kinase [VEGFR2(KDR)/VEGFR3(Flt-4)]inhibitorwith potential antitumor activity. |
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V3700 | Lenvatinib mesylate | 857890-39-2 | Lenvatinib mesylate (also known as E-7080, E7080,ER-203492-00;Lenvima), themesylate salt of lenvatinib, is a multi-targeted and orally bioavailable inhibitor of VEGFR2(KDR)/VEGFR3(Flt-4)approved in 2015 for the treatment of differentiated thyroid cancer. |
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V0529 | Linifanib (ABT-869; AL-39324) | 796967-16-3 | Linifanib (formerly RG3635, ABT869, AL39324) is an orally bioavailable and ATP-competitive inhibitor of multiple kinases (e. |
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V5020 | Lucitanib (E3810) | 1058137-23-7 | Lucitanib (formerly E3810; AL3810; E-3810) is a novel and potent dual VEGFR and FGFR inhibitor with anticancer effects. |
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V0499 | LY2874455 | 1254473-64-7 | LY2874455 (LY-2874455; LY 2874455) is a novel and highly potent pan-FGFR inhibitor with potential anticancer activity. |
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V2187 | MAZ51 | 163655-37-6 | Decsription: MAZ-51 is a novel, potent and selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. |
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