Anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase in the insulin receptor superfamily, is predominantly expressed in the brain and implicated in neuronal development and cognition. Adenosine triphosphate (ATP) and a gamma-phosphate group are transferred via ALK to a tyrosine residue on a substrate protein. As a result, it causes the tyrosine residues in its substrate proteins to phosphorylate. Different enzymes (kinases and phosphatases) catalyze the important protein reactions of phosphorylation and dephosphorylation, which are essential to many cellular processes.
ALK gene activation results from fusion with other oncogenes (NPM, EML4, TIM, etc.) or gene amplification, mutation, or protein overexpression and contributes to the development of several human cancers, including anaplastic large cell lymphoma, lung cancer, inflammatory myofibroblastic tumors, and neuroblastoma. ALK is a transmembrane tyrosine kinase receptor that dimerizes and then autophosphorylates the intracellular kinase domain in response to ligand binding to its extracellular domain. Specific inhibitors, like Crizotinib, Ceritinib, Alectinib, etc., have shown to be highly effective in treating ALK-positive non-small cell lung cancer in particular when it becomes activated in cancer.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V0613 | Loratinib (PF-06463922; Lorlatinib; lorbrena) | 1454846-35-5 | Loratinib (formerly also known as Lorlatinib, PF-06463922; trade name:Lorbrena) is a potent, orally bioavailable, brain-penetrant,ATP-competitive, anddual ALK/ROS1 inhibitor with potential antitumor activity. |
|
V3573 | MS4078 | 2229036-62-6 | MS4078 is a potent PROTACdegrader of anaplastic lymphoma kinase (ALK)with aKdof 19 nM for binding affinity to ALK. |
|
V14334 | SAR348830 | 1462949-64-9 | SAR348830 (SAR-348830; SAR 348830) is potent and selective inhibitor of anaplastic lymphoma kinase (ALK ) with the potential to be used for treatingNon-small Cell Lung Cancer. |
|
V0605 | TAE684 (NVP-TAE684) | 761439-42-3 | TAE684 (also called NVP-TAE684; TAE-684) is a novel, highly potent and selective small-molecule inhibitor of the ALK (anaplastic lymphoma kinase) tyrosine kinase with potential anticancer activity. |
|
V2490 | Zotizalkib (TPX-0131) | 2648641-36-3 | TPX 0131 (TPX-0131) is a novel, potent CNS-penetrant ALK inhibitor with anticancer activity. |
|
V39663 | ZX-29 | 2254805-62-2 | ZX-29 is a potent and specific ALK inhibitor (antagonist) with IC50s of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R respectively, but has no activity against EGFR. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
