ALK

ALK

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.

ALK related products

Structure Cat No. Product Name CAS No. Product Description
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.
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.
V3324 ALK inhibitor 2 761438-38-4 ALK inhibitor 2 is a novel, potent and selective inhibitor for the ALK kinase (anaplastic lymphoma kinase).
V0612 ASP3026 1097917-15-1 ASP3026 (ASP-3026; ASP 3026) is an orally bioavailable inhibitor of ALK (anaplastic lymphoma kinase) with potential antineoplastic activity.
V0611 AZD3463 1356962-20-3 AZD-3463 (AZD3463) is a novel, potent and selective ALK/IGF1R inhibitor with potential anticancer activity.
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.
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.
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).
V78550 Brigatinib-13C6 (AP-26113-13C6)
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.
V77157 CEP-28122 mesylate salt
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.
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).
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.
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.
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.
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.
V0608 GSK1838705A 1116235-97-2 GSK1838705A (GSK-1838705A) is a novel, potent and reversible small-molecule IGF-1R inhibitor with potential anticancer activity.
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).
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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