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)

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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-50878
    Crizotinib
    		Inhibitor 99.97%
    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
  • HY-12215
    Lorlatinib
    		Inhibitor 99.99%
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALKL1196), 14-80 nM (ALKG1269A), 38-50 nM (ALK1151Tins), 77-113 nM (ALKG1202R), respectively.
    Lorlatinib
  • HY-12678
    Entrectinib
    		Inhibitor 99.79%
    Entrectinib (NMS-E628) 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
  • HY-15656
    Ceritinib
    		Inhibitor 99.95%
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency.
    Ceritinib
  • HY-13011
    Alectinib
    		Inhibitor 99.78%
    Alectinib (CH5424802; RO5424802; RG7853) 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
  • HY-183116
    TRI-611
    		Degrader 99.07%
    TRI-611 is a brain-penetrant, orally active molecular glue degrader targeting ALK. TRI-611 engages ALK via a distal degron, forms a ternary complex with CRBN, triggers ALK polyubiquitination and degradation, including TKI-resistant ALK fusion proteins. TRI-611 inhibits ALK downstream signaling pathways, induces anti-proliferative effects in ALK-positive cancer cells. TRI-611 induces regression of ALK-positive non-small cell lung cancer tumors in preclinical xenograft models. TRI-611 can be used for the research of ALK-positive non-small cell lung cancer, including TKI-refractory tumors and central nervous system metastases.
    TRI-611
  • HY-149591
    M4K-2009
    		Inhibitor 99.35%
    M4K-2009 is an orally bioactive ALK2 inhibitor with an IC50 of 13 nM. M4K-2009 exerts comparable inhibitory potency against wild-type and mutant ALK2G328V, ALK2R206H, and ALK2R258G. M4K-2009 exhibits moderate off-target inhibitory activity against hERG potassium channels. M4K-2009 can be used in studies related to diffuse intrinsic pontine glioma.
    M4K-2009
  • HY-183718
    M4K3250
    		Degrader
    M4K3250 is a selective ALK2 PROTAC degrader with a pDC50 of 7.9. M4K3250 induces the formation of a ternary complex between ALK2 and the E3 ubiquitin ligase CRBN, thereby causing ALK2 degradation and inhibiting ALK2 activity. M4K3250 exhibits cytotoxicity in glioblastoma cells. M4K3250 can be used in studies related to glioblastoma.
    M4K3250
  • HY-12857
    Brigatinib
    		Inhibitor 99.98%
    Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC50 of 0.6 nM. Brigatinib can be used for research of NSCLC.
    Brigatinib
  • HY-103022
    Repotrectinib
    		Inhibitor 99.95%
    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.
    Repotrectinib
  • HY-155489
    DDO-2728
    		Inhibitor 98.64%
    DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N6 methyladenosine (m6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4 11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research.
    DDO-2728
  • HY-15656A
    Ceritinib dihydrochloride
    		Inhibitor 99.90%
    Ceritinib (LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride shows great antitumor potency.
    Ceritinib dihydrochloride
  • HY-13011A
    Alectinib Hydrochloride
    		Inhibitor 99.92%
    Alectinib (CH5424802; RO5424802; RG7853) Hydrochloride 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 Hydrochloride
  • HY-156467
    Neladalkib
    		Inhibitor 99.90%
    Neladalkib (NVL-655) is an oral ALK inhibitor, the IC50 for Neladalkib in inhibiting ALK is 2.8 nM. Neladalkib promotes cell apoptosis and has anti-tumor activity.
    Neladalkib
  • HY-10192
    NVP-TAE 684
    		Inhibitor 99.70%
    NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.
    NVP-TAE 684
  • HY-50878A
    Crizotinib hydrochloride
    		Inhibitor 99.86%
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.
    Crizotinib hydrochloride
  • HY-132200
    UNC5293
    		Inhibitor 99.93%
    UNC5293 is a MERTK-selective and potent inhibitor (Ki=190 pM). UNC5293 inhibits MERTK (IC50=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research.
    UNC5293
  • HY-15609
    AZD-3463
    		Inhibitor 99.31%
    AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells.
    AZD-3463
  • HY-112155
    MS4078
    		Inhibitor 99.72%
    MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19?nM for binding affinity to ALK.
    MS4078
  • HY-12953
    R-268712
    		Inhibitor 99.92%
    R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.
    R-268712
Cat. No. Product Name / Synonyms Application Reactivity