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
1419 AB 1010 PDGFR, c-KIT and FGFR3 tyrosine kinase inhibitor €70.00
1638 ABT 869 PDGFR, c-KIT and VEGFR tyrosine kinase inhibitor €85.00
1696 AC 220 dihydrochloride FLT3 inhibitor €90.00
1653 AEE 788 EGFR, ErbB2 and VEGFR tyrosine kinase inhibitor €95.00
1414 AG 013736 PDGFR,c-KIT and VEGFR tyrosine kinase inhibitor €75.00
1916 AMG 208 Inhibitor of c-MET receptor tyrosine kinase (RTK) €110.00
1768 AMG 706 Multiple receptor tyrosine kinase inhibitor €105.00
2368 Amuvatinib RTK inhibitor which effectively inhibits PDGFR, c-Kit and c-Met €105.00
2468 ANA 12 Selective TrkB antagonist with anxiolytic and antidepressant activity in mice €90.00
1838 ARQ 197 c-MET tyrosine kinase Inhibitor €95.00
1986 AST 1306 tosylate ErbB2 and EGFR inhibitor €105.00
1610 AZ 23 TrkA and TrkB inhibitor €90.00
2153 AZD 3463 Potent inhibitor of ALK and IGF1R €105.00
2563 AZD 3759 Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor €85.00
1917 AZD 4547 Potent and selective FGFR inhibitor €85.00

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