1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)

Anaplastic lymphoma kinase (ALK)

Anaplastic lymphoma kinase; ALK tyrosine kinase receptor; CD246; Cluster of differentiation 246

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. ALK catalyzes the transference of a gamma-phosphate group from adenosine triphosphate (ATP) to a tyrosine residue on a substrate protein. Therefore, it catalyzes a tyrosine residue phosphorylation reaction on its substrate proteins. The phosphorylation and dephosphorylation of proteins are critical reactions catalyzed by different enzymes (kinases and phosphatases), which play critical roles in various cellular functions.

ALK gene activation is involved in the carcinogenesis process of several human cancers such as anaplastic large cell lymphoma, lung cancer, inflammatory myofibroblastic tumors and neuroblastoma, as a consequence of fusion with other oncogenes (NPM, EML4, TIM, etc) or gene amplification, mutation or protein overexpression. ALK is a transmembrane tyrosine kinase receptor that, upon ligand binding to its extracellular domain, undergoes dimerization and subsequent autophosphorylation of the intracellular kinase domain. When activated in cancer it represents a target for specific inhibitors, such as Crizotinib, Ceritinib, Alectinib etc. which use has demonstrated significant effectiveness in ALK-positive non-small cell lung cancer particularly.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18030B
    CEP-28122 mesylate hydrochloride
    Inhibitor
    CEP-28122 mesylate hydrochloride is a diaminopyrimidine derivative.CEP-28122 mesylate hydrochloride is a potent, selective, and orally bioavailable ALK inhibitor with an IC50 of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor and good pharmacokinetic activity.
    CEP-28122 mesylate hydrochloride
  • HY-50878R
    Crizotinib (Standard)
    Inhibitor
    Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
    Crizotinib (Standard)
  • HY-169481
    AP-1
    Degrader
    AP-1 is a PROTAC targeting anaplastic lymphoma kinase (ALK). AP-1 is composed of PROTAC target protein ligand CS-1243648 (HY-169482) (red part), E3 ligase ligand Pomalidomide (HY-10984) (blue part) and PROTAC Linker 2-(Tert-Butoxy)-2-oxoacetic acid (HY-W687662) (black part).
    AP-1
  • HY-13011R
    Alectinib (Standard)
    Inhibitor
    Alectinib (Standard) is the analytical standard of Alectinib. This product is intended for research and analytical applications. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
    Alectinib (Standard)
  • HY-W814315
    Alectinib analog
    Alectinib analog (CH5424802 analog) is a selective ALK inhibitor with activity in blocking resistance gating mutations. The synthetic optimization of alectinib analog allows it to be combined with specific peptides to improve the ability to target cancer cells. Alectinib analog exhibits low micromolar IC50 values in antiproliferation and shows good cytotoxic effects. The inhibitory activity of alectinib analog is closely related to its stability and release of active ingredients. Alectinib analog demonstrated the ability to inhibit vascular septal length or width in an in vivo zebrafish model.
    Alectinib analog
  • HY-13464R
    ALK-IN-1 (Standard)
    Inhibitor
    ALK-IN-1 (Standard) is the analytical standard of ALK-IN-1. This product is intended for research and analytical applications. ALK-IN-1 (Brigatinib analog) is a highly efficient and selective inhibitor of ALK kinase, derived from patent US20140066406 A1.
    ALK-IN-1 (Standard)
  • HY-13326R
    ASP3026 (Standard)
    Inhibitor
    ASP3026 (Standard) is the analytical standard of ASP3026. This product is intended for research and analytical applications. ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research.
    ASP3026 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity