1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. ALK

ALK

ALK (Anaplastic lymphoma kinase) is encoded by the ALK gene. ALK is a membrane associated tyrosine kinase receptor of the insulin receptor superfamily. The function of the full-length ALK receptor is poorly understood. It has a probable role in the central and peripheral nervous system development and maintenance. ALK is a dependence receptor, which may exert antagonist functions, proapoptotic or antiapoptotic, depending on the absence or presence of a ligand. Dependence receptors have a potential role in cancer and development. Ligands available for this demonstration were agonist anti-ALK antibodies. ALK is still an orphan receptor, given the high level of controversy about pleiotrophin and midkine.

ALK Related Products (41):

Cat. No. Product Name Effect Purity
  • HY-50878
    Crizotinib Inhibitor 99.97%
    Crizotinib (PF-02341066) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib (PF-02341066) 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 (PF-02341066) is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib (PF-02341066) has effective tumor growth inhibition.
  • HY-12857
    Brigatinib Inhibitor 99.98%
    Brigatinib is a highly potent and selective ALK inhibitor, with an IC50 of 0.6 nM.
  • HY-12215
    Lorlatinib Inhibitor 99.83%
    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.
  • HY-13011
    Alectinib Inhibitor 99.84%
    Alectinib (CH5424802; RO5424802; AF802) 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.
  • HY-12678
    Entrectinib Inhibitor 99.32%
    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-100444
    SIS3 free base Inhibitor
    SIS3 free base is a potent and selective inhibitor of TGF- beta1-induced Smad3 phosphorylation with an IC50 of 3 μM. SIS3 free base increases luciferase activity of p3TP-lux by abrogating the overexpression of constitutively active form of ALK-5.
  • HY-122582
    TL13-12 Inhibitor
    TL13-12 is a potent ALK-PROTAC degrade comprised by conjugation of TAE684 (HY-10192) and the cereblon ligand pomalidomide (HY-10984). TL13-12 inhibits ALK activity an IC50 value of 0.69 nM, and also prompt the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 withIC50 values of 13.5 nM, 5.74 nM, 18.4 nM and 65 nM, respectively.
  • HY-125851
    TGFβRI-IN-2 Inhibitor
    TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
  • HY-15656
    Ceritinib Inhibitor 99.98%
    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.
  • HY-10192
    NVP-TAE 684 Inhibitor 99.40%
    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.
  • HY-103022
    Repotrectinib Inhibitor 99.91%
    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor. Repotrectinib (TPX-0005) potently inhibits WT ALK (1.01 nM) and mutant ALKs including ALK G1202R (1.26 nM) and ALK L1196M (1.08 nM). It also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (1.04, 1.66, 5.3, and 6.96 nM, respectively) .
  • 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.
  • HY-15656A
    Ceritinib dihydrochloride Inhibitor 99.98%
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
  • HY-103714A
    Ensartinib hydrochloride Inhibitor 98.51%
    Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  • HY-13011A
    Alectinib Hydrochloride Inhibitor 99.95%
    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. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-13020
    GSK1838705A Inhibitor 99.28%
    GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
  • HY-13464
    ALK-IN-1 Inhibitor 99.96%
    ALK-IN-1 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.
  • HY-15609
    AZD-3463 Inhibitor 98.49%
    AZD-3463 is an ALK/IGF1R inhibitor which overcomes multiple mechanisms of acquired resistance to crizotinib.
  • HY-16590
    X-376 Inhibitor 98.36%
    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.
  • HY-15841
    CEP-37440 Inhibitor 99.87%
    CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).
Isoform Specific Products

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