ALK
As a result of their high degree of similarity, Anaplastic Lymphoma Kinase (ALK, RTK class XIX, LTK receptor family) and Leukocyte Tyrosine Kinase (LTK) were originally identified as a member of the ros/insulin receptor subfamily of receptor tyrosine kinases[1]. ALK was first discovered as the constitutively active nucleophosmin NPM-ALK oncoprotein in anaplastic large cell lymphomas (ALCL). Full length ALK is abundantly expressed in neural tissue during embryogenesis, but levels fall during early development. Consequently, it has been hypothesized to play a critical role in normal development and differentiation of the central and peripheral nervous system[2]. ALK fusions derived from gene translocations are associated with large cell lymphomas and inflammatory myofibrilastic tumors.
[1] ALK, the chromosome 2 gene locus altered by the t(2;5) in non-Hodgkin's lymphoma, encodes a novel neural receptor tyrosine kinase that is highly related to leukocyte tyrosine kinase (LTK). S.W. Morris, C. Naeve, P. Mathew, P.L. James, M.N. Kirstein, X. Cui, D.P. Witte. Oncogene 1997, 14, 2175-2188.
[2] ALK inhibitors, a pharmaceutical perspective. E. Ardini, A. Galvani. Front. Oncol. 2012, 17, 1-8.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 1884 | Alectinib | Orally available and selective ALK inhibitor | €70.00 | |
| 2153 | AZD3463 | Potent inhibitor of ALK and IGF1R | €105.00 | |
| 2978 | Brigatinib | Potent, selective, and orally active anaplastic lymphoma kinase (ALK) inhibitor | €80.00 | |
| 2267 | GSK 1838705A | Potent IGF-IR and insulin receptor (IR) kinase inhibitor with additional affinity for ALK | €110.00 | |
| 2224 | LDK 378 | Potent, bioavailable, and selective anaplastic lymphoma kinase (ALK) inhibitor | €95.00 | |
| 2600 | PF 06463922 | Potent, orally available and brain-penetrant ALK/ROS1 selective inhibitor | €105.00 | |