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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V32937 | Crizotinib HCl | 1415560-69-8 | Crizotinib HCl (formerly known as PF-02341066 hydrochloride; trade name: Xalkori) is a potent, orally bioavailable small molecule inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. |
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V31650 | Ensartinib hydrochloride ( X396) | 2137030-98-7 | Ensartinib (formerly known as X-396) is a novel, highlypotent, selective,andorally available small molecule inhibitor of ALK (anaplastic lymphoma kinase) with an IC50 less than 4 nM in Ambit assays. |
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V0154 | Ceritinib (LDK-378; Zykadia) | 1032900-25-6 | Ceritinib (formerly known as LDK378; tradename: Zykadia) is novel, potent and selectiveinhibitor against ALK (anaplastic lymphoma kinase positive) with potential anticancer activity. |
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V0070 | Alectinib HCl (ALECENSA, AF-802, CH-5424802, RO-5424802) | 1256589-74-8 | Alectinib HCl (formerly AF802, CH5424802 or RO5424802; trade name ALECENSA) is a potent, selective, and orally bioavailable inhibitor of ALK (anaplastic lymphoma kinase) tyrosine kinase with IC50 value of 1.9 nM in cell-free assays. |
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V2755 | Belizatinib | 1357920-84-3 | Belizatinib, formerly known as TSR-011, isa potent,orally bioavailable dual inhibitor ofALK (anaplastic lymphoma kinase) with IC50 of 0.7 nM and an inhibitor oftropomyosin receptor kinase (TRK)with IC50 values less than 3 nM for TRK A, B, and C. |
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V0606 | Alectinib (AF-802, CH-5424802, RO-5424802, Alecensa) | 1256580-46-7 | Alectinib (formerly AF802, CH5424802, RO5424802; trade name Alecensa) is a potent, selective, and orally bioavailable ALK (anaplastic lymphoma kinase) tyrosine kinase inhibitor with potential antitumor activity. |
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