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

Anaplastic lymphoma kinase (ALK)

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

Anaplastic lymphoma kinase (ALK)

Related Products

PDF 0.92 MB

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-16590
    X-376
    		Inhibitor 98.37%
    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
    X-376
  • HY-112801
    F-1
    		Inhibitor 98.65%
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively.
    F-1
  • HY-122582
    TL13-12
    		Inhibitor 98.06%
    TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984).
    TL13-12
  • HY-152845
    Ficonalkib
    		Inhibitor 98.55%
    Ficonalkib is a potent inhibitor of Anaplastic lymphoma kinase (ALK), the tyrosine kinase receptor. Ficonalkib, can be used as an antineoplastic agent.
    Ficonalkib
  • HY-145566
    Envonalkib
    		Inhibitor 99.73%
    Envonalkib is a potent and orally active inhibitor of ALK, with IC50s of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK. Envonalkib can be used for the research of non-small cell lung cancer.
    Envonalkib
  • HY-160520
    ALK-IN-28
    		Inhibitor 98.49%
    ALK-IN-28 (compound 22) is an inhibitor of anaplastic lymphoma kinase (ALK).
    ALK-IN-28
  • HY-147219A
    SIAIS164018 hydrochloride
    		Inhibitor 99.84%
    SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857).
    SIAIS164018 hydrochloride
  • HY-N4126
    6-Demethoxytangeretin
    		Inhibitor 99.37%
    6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus reticulata. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons.
    6-Demethoxytangeretin
  • HY-156467
    ALK-IN-27
    		Inhibitor 99.90%
    ALK-IN-27 (compound 1) is a potent ALK inhibitor. ALK-IN-27 shows antitumor activity. ALK-IN-27 has an IC50 of 2.7 nM for Ba/F3 CLIP1-LTK cells.
    ALK-IN-27
  • HY-111752
    EML4-ALK kinase inhibitor 1
    		Inhibitor 98.49%
    EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
    EML4-ALK kinase inhibitor 1
  • HY-112140
    JH-VIII-157-02
    		Inhibitor 99.67%
    JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.
    JH-VIII-157-02
  • HY-10432G
    A 83-01 (GMP)
    		Inhibitor
    A 83-01 (GMP) is A 83-01 (HY-10432) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. A 83-01 is a potent ALK4/5/7 inhibitor.
    A 83-01 (GMP)
  • HY-147219
    SIAIS164018
    		Inhibitor
    SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857).
    SIAIS164018
  • HY-15656S
    Ceritinib-d7
    		Inhibitor 98.00%
    Ceritinib-d7 is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor[1].
    Ceritinib-d<sub>7</sub>
  • HY-135887
    ZX-29
    		Inhibitor 99.52%
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
    ZX-29
  • HY-12678S
    Entrectinib-d4
    		Inhibitor
    Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.
    Entrectinib-d<sub>4</sub>
  • HY-103714
    Ensartinib
    		Inhibitor
    Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
    Ensartinib
  • HY-18030
    CEP-28122
    		Inhibitor
    CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.
    CEP-28122
  • HY-50878B
    Crizotinib acetate
    		Inhibitor
    Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate 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 acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition.
    Crizotinib acetate
  • HY-128569
    ALK-IN-5
    		Inhibitor
    ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK), with an IC50 of 2.9 nM.
    ALK-IN-5
Cat. No. Product Name / Synonyms Application Reactivity