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
2563 AZD 3759 Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor €85.00
1917 AZD 4547 Potent and selective FGFR inhibitor €85.00
2342 AZD 9291 Potent oral, irreversible, third-generation EGFR TKI with selectivity for mutant EGFRs €95.00
1544 BIBW 2992 EGFR and ErbB-2/HER2 tyrosine kinase inhibitor €65.00
1850 BMS 540215 Inhibitor of VEGFR (subtype 2 and 3 selective) €110.00
2837 BMS 605541 Potent, selective, orally active, and ATP-competitive VEGFR2 inhibitor €90.00
2978 Brigatinib Potent, selective, and orally active anaplastic lymphoma kinase (ALK) inhibitor  Recently added €80.00
1864 Brivanib alaninate Prodrug of BMS 540215; Inhibitor of VEGF €105.00
1819 Cabozantinib S-malate Inhibitor of multiple receptor tyrosine kinases, specifically MET and VEGFR2 €85.00
1461 Cediranib VEGFR tyrosine kinase inhibitor €70.00
1884 CH 5424802 Orally available and selective ALK inhibitor €95.00
1433 CI 1033 EGFR tyrosine kinase inhibitor €60.00
2061 CID 11654378 Potent FMS kinase inhibitor €135.00
1662 CP 547632 VEGFR2 tyrosine kinase inhibitor €105.00
1537 CP 724714 ErbB-2/HER2 kinase inhibitor €80.00

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