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 |
|---|---|---|---|---|
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V3324 | ALK inhibitor 2 | 761438-38-4 | ALK inhibitor 2 is a novel, potent and selective inhibitor for the ALK kinase (anaplastic lymphoma kinase). |
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V0612 | ASP3026 | 1097917-15-1 | ASP3026 (ASP-3026; ASP 3026) is an orally bioavailable inhibitor of ALK (anaplastic lymphoma kinase) with potential antineoplastic activity. |
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V0611 | AZD3463 | 1356962-20-3 | AZD-3463 (AZD3463) is a novel, potent and selective ALK/IGF1R inhibitor with potential anticancer activity. |
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V78550 | Brigatinib-13C6 (AP-26113-13C6) | Brigatinib-13C6 is a 13C (carbon 13)-labeled Brigatinib. | |
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V17903 | CEP-28122 | 1022958-60-6 | CEP-28122 is a novel, potent, selective and orally bioavailable ALK inhibitor with a favorable pharmacodynamic and pharmacokinetic profile and robust and selective pharmacologic efficacy against ALK-positive human cancer cells and tumor xenograft models in mice. |
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V77157 | CEP-28122 mesylate salt | 2070009-30-0 | CEP-28122 mesylate salt is a diaminopyrimidine analogue that is a specific and orally bioactive ALK inhibitor (antagonist) with IC50 of 1.9 nM for recombinant ALK kinase activity. |
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V0608 | GSK1838705A | 1116235-97-2 | GSK1838705A (GSK-1838705A) is a novel, potent and reversible small-molecule IGF-1R inhibitor with potential anticancer activity. |
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V3374 | HG-14-10-04 | 1356962-34-9 | HG-14-10-04 is a novel, potent and specific ALK (Anaplastic lymphoma kinase) inhibitor with IC50 of 20The anaplastic lymphoma kinase (ALK) gene plays an important physiologic role in the development of the brain and can be oncogenically altered in several malignancies, including non-small-cell lung cancer (NSCLC) and anaplastic large cell lymphomas (ALCL). |
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V23301 | KRCA-0008 | 1472795-20-2 | KRCA-0008 is a novel, potent dual inhibitor of Ack1 and anaplastic lymphoma kinase (ALK)with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability. |
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V3573 | MS4078 | 2229036-62-6 | MS4078 is a potent PROTACdegrader of anaplastic lymphoma kinase (ALK)with aKdof 19 nM for binding affinity to ALK. |
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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. |
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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. |
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V2490 | Zotizalkib (TPX-0131) | 2648641-36-3 | TPX 0131 (TPX-0131) is a novel, potent CNS-penetrant ALK inhibitor with anticancer activity. |
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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. |
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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. |
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V17933 | Ceritinib diHCl | 1380575-43-8 | Ceritinib diHCl (LDK-378; LDK378; Zykadia; Spexib), the dihydrochloride salt of ceritinib, is an ALK (anaplastic lymphoma kinase positive) inhibitor approved in 2014 for the treatment of non-small cell lung cancer (NSCLC). |
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V3921 | BRIGATINIB ANALOG | 1197958-12-5 | Brigatinib analog is a derivative of Brigatinib (AP-26113; Alunbrig), which is an orally bioavailable ALK (anaplastic lymphoma kinase) inhibitor approved by FDA in 2017 for the treatment of ALK-positive metastatic non-small cell lung cancer (NSCLC). |
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V0607 | Brigatinib (AP26113) | 1197953-54-0 | Brigatinib (formerly AP26113;AP-26113; ALK-IN-1; trade name:Alunbrig) is an orally bioavailable, FDA-approved and selective ALK (anaplastic lymphoma kinase) inhibitor with potential antineoplastic activity. |
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V0609 | Entrectinib (NMS-E 628; RXDX101; ROZLYTREK) | 1108743-60-7 | Entrectinib (formerly also known as NMS-E628; RXDX-101; trade nameROZLYTREK) is a potent and orally bioavailable small molecule inhibitor of TrkA, TrkB, TrkC, ROS1 and ALK with potential antitumor activity. |
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V2779 | Ensartinib | 1370651-20-9 | Ensartinib (formerly known as X-396) is a novel, highlypotent andselective,orally available small molecule inhibitor of ALK (anaplastic lymphoma kinase) with an IC50 less than 4 nM in Ambit assays. |
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