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

Anaplastic lymphoma kinase (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. 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.

Anaplastic lymphoma kinase (ALK) Related Products (73):

Cat. No. Product Name Effect Purity
  • 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[1][2][3].
  • HY-12215
    Lorlatinib Inhibitor
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M, respectively. Lorlatinib has anticancer activity[1][2].
  • HY-12678
    Entrectinib Inhibitor 99.83%
    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.
  • HY-13011
    Alectinib Inhibitor 99.87%
    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[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
  • HY-15656
    Ceritinib Inhibitor 99.97%
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency[1][2].
  • HY-P99353
    Ascrinvacumab Inhibitor
    Ascrinvacumab (PF-03446962) is a human IgG2 monoclonal antibody targets ALK-1. Ascrinvacumab shows binding efficiency with human ALK1 with a Kd value of 7 nM. Ascrinvacumab can be used for the research of hepatocellular carcinoma (HCC)[1].
  • 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[1][2].
  • HY-152845
    Ficonalkib Inhibitor
    Ficonalkib is a potent inhibitor of Anaplastic lymphoma kinase (ALK), the tyrosine kinase receptor. Ficonalkib, can be used as an antineoplastic agent[1][2].
  • HY-137506
    XST-14 Inhibitor 99.69%
    XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects[1].
  • HY-15609
    AZD-3463 Inhibitor 99.96%
    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[1][2][3].
  • HY-12857S
    Brigatinib-13C6 Inhibitor
    Brigatinib-13C6 is the 13C-labeled Brigatinib. Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC50 of 0.6 nM[1].
  • HY-12857
    Brigatinib Inhibitor 99.98%
    Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC50 of 0.6 nM[1].
  • HY-13011S1
    Alectinib-d6 Inhibitor
    Alectinib-d6 is deuterium labeled Alectinib. 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[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
  • HY-15841
    CEP-37440 Inhibitor 99.58%
    CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397)[1][2].
  • HY-17603
    Belizatinib Inhibitor 99.64%
    Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
  • HY-130794
    ALK/ROS1-IN-1 Inhibitor
    ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
  • HY-144732
    TRK/ALK-IN-1 Inhibitor
    TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALKWT and ALKL1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases[1].
  • HY-103714A
    Ensartinib dihydrochloride Inhibitor 99.53%
    Ensartinib dihydrochloride (X-396 dihydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  • HY-13011A
    Alectinib Hydrochloride Inhibitor 99.93%
    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 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[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
  • 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[1].