RTK

Many of the Axon Ligands™ in this class of compounds target receptors of various growth factors, such as EGF, VEGF, and PDGF. These receptors are members of the class of enzyme linked receptors, which, as integral membrane proteins, possess both receptor functionality (extra-cellular) as well as enzymatic catalytic functionality (intracellular)[1],[2]. The majority of the enzymatic activity of this class of receptors is characterized by kinase-like activity. Based on this feature, five main classes can be distinguished[3]: Receptor Tyrosine Kinases (RTKs), and Receptor Serine/Threonine Kinases (RSTKs, participating in MAPK and TGF-beta signaling pathways, among others) are well known. Additionally, there are classes of Receptor Guanylyl Cyclases, Histidine Kinase associated Receptors (receptors that associate with proteins that have histidine kinase activity), and finally a class of Tyrosine Kinase associated Receptors (e.g. Cytokine Receptors). In addition, some transmembrane tyrosine phosphatases (Receptor-like) Protein Tyrosine Phosphatases (PTPs)), which remove phosphate from phosphotyrosine side chains of specific proteins, are thought to function as receptors, although for the most part their ligands are unknown. Within each of these main classes, sub-classes exist, based on the specific endogenous ligands. Many of the enzyme linked receptors play a role in the regulation of cell proliferation, programmed cell death (apoptosis), cell differentiation, and embryonic development, and therefore are of great interest as targets for the treatment of cancer[4]. Furthermore, malfunctioning of receptors of this kind is associated with the development of neurodegenerative diseases, such as multiple sclerosis and Alzheimer's disease[5].


[1] Catalytic Receptors. S.P.H. Alexander, A. Mathie, and J.A. Peters. Br. J. Pharmacol. 2007, 150(S1): S122–S127. 
[2] Cell Signaling by Receptor Tyrosine Kinases. M.A. Lemmon, J. Schlessinger. Cell 2010, 141, 1117-1134.
[3] Molecular Biology of the Cell. 4th edition. Alberts B, Johnson A, Lewis J, et al.New York:Garland Science; 2002.
[4] Tyrosine kinase receptors as attractive targets of cancer therapy. Bennasroune A, Gardin A., Aunis D., Crémel G., Hubert P. Crit. Rev. Oncol. Hematol. 2004, 50, 23-38.
[5] The EGF receptor family: spearheading a merger of signaling and therapeutics. Bublil E.M., Yarden Y. Curr. Opin. Cell Biol. 2007, 19,124-134.

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Axon ID Name Description From price
1978 ZM 323881 hydrochloride Inhibitor of VEGFR2 €105.00
1506 WZ 4002 EGFR kinase inhibitor (T790M specific) €70.00
1637 Vatalanib VEGFR tyrosine kinase inhibitor €75.00
1411 Vandetanib VEGFR and EGFR tyrosine kinase inhibitor €55.00
2086 UNC 569 Reversible and ATP-competitive inhibitor of Mer (RTK) €95.00
2346 UNC 2250 Potent Mer kinase inhibitor with promising selectivity and PK properties. €80.00
1717 Tivozanib VEGFR1, 2, and 3 tyrosine kinase inhibitor €99.00
2053 TAK 165 ErbB2/HER2 kinase inhibitor €65.00
1398 Sunitinib malate Multi-targeted receptor tyrosine kinase inhibitor €80.00
2767 SU11652 Multi-targeted receptor tyrosine kinase inhibitor €145.00
1891 SU 6668 Inhibitor of RTK targeting PDGFR, VEGF and FGFR €105.00
1667 SU 5402 Fibroblast growth factor receptor (FGFR) inhibitor €65.00
1581 SU 11274 ATP-competitive inhibitor of c-MET €95.00
5006 Stem Cell CSD inhibitor Set Set of CHIR 99021, SU5402, and DAPT, inhibitors of GSK-3, FGFR, and γ-secretase, resp. €155.00
5007 Stem Cell 5i inhibitor Set Set of five inhibitors for neural differentiation of human pluripotent stem cells. €220.00

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