ALK

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  1. TRK, ROS1, ALK inhibitor

    Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.
  2. ALK4/ALK5 inhibitor

    EW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively
  3. c-Met/NPM-ALK inhibitor

    Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.
  4. ALK inhibitor

    LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.
  5. ALK Inhibitor

    Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
  6. ALK inhibitor

    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.
  7. ALK/ c-Met inhibitor

    PF-2341066 (Crizotinib) is an inhibitor of the c-Met kinase and the NPM-ALK. PF-2341066 inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM).
  8. BMP inhibitor

    DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).
  9. IGF-1R Inhibitor

    GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively.

  10. ALK Inhibitor

    TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant).
  11. TGF-β/ALK5 inhibitor

    A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7
  12. ALK/IGF1R inhibitor

    AZD-3463 is a ALK/IGF1R inhibitor.
  13. ALK Inhibitor

    LDK378 is a highly selective, orally bioavailable and ATP-competitive small molecule inhibitor of ALK (Anaplastic Lymphoma Kinase), a receptor tyrosine kinase considered to be an important lung cancer drug target.
  14. ALK Inhibitor

    Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK.

  15. ALK5 inhibitor

    SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively).
  16. ALK inhibitor

    ASP3026 is a novel and selective inhibitor for the ALK kinase. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel.
  17. ALK inhibitor

    ALK-IN-1, an analog of AP26113, is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line.

  18. Alk2 inhibitor

    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
  19. ALK inhibitor

    CEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
  20. ALK inhibitor

    Lorlatinib (PF-06463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively.

  21. NUAK kinase inhibitor

    WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2
  22. ALK5 inhibitor

    A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
  23. ALK2 inhibitor

    LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM.
  24. ALK5 inhibitor

    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  25. ALK/EGFR inhibitor

    HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
  26. ALK/TRKA/TRKB/TRKC inhibitor

    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.
  27. ALK inhibitor

    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.
  28. ALK/MET inhibitor

    Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  29. ALK5/ALK4 inhibitor

    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
  30. ALK/ ROS1 dual inhibitor

    WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
  31. ALK PROTAC degrader

    MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37?nM for binding affinity to ALK.
  32. ALK PROTAC degrader

    MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19?nM for binding affinity to ALK.
  33. ALK inhibitor

    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.
  34. F-1

    ALK and ROS1 dual inhibitor

    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.
  35. ALK inhibitor

    ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
  36. ALK inhibitor

    ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.
  37. ALK inhibitor

    LDK378 dihydrochloride is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
  38. ACK1/ALK inhibitor

    KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.
  39. FAK/ALK inhibitor

    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).
  40. ALK inhibitor

    ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively.
  41. ALK/FAK/ROS1 Multikinase Inhibitor

    APG-2449 is an orally active inhibitor targeting BCL-2 and multikinase pathways, specifically ALK, FAK, and ROS1. It demonstrates potent antitumor activity by reducing cell viability and enhancing apoptosis in acute myeloid leukemia cells in vitro. APG-2449 effectively decreases the activation of FAK and its downstream signaling effectors. This compound is suitable for research applications in various malignancies, including mesothelioma, non-small cell lung cancer, ovarian cancer, and other hematologic and solid tumors.
  42. ALKBH5 Inhibitor

    W23-1006 is a selective and covalent inhibitor of ALKBH5, targeting the C200 residue with an IC50 of 3.848 μM. This compound exhibits approximately 30-fold and 8-fold greater inhibitory activity against ALKBH5 compared to FTO and ALKBH3, respectively. W23-1006 is particularly valuable for research applications focusing on triple-negative breast cancer (TNBC), enabling studies on the role of ALKBH5 in tumor biology and potential therapeutic strategies.
  43. ALK Tyrosine Kinase Inhibitor

    Ceritinib-d7 is a deuterium-labeled derivative of Ceritinib, which functions as a selective and ATP-competitive inhibitor of the ALK (anaplastic lymphoma kinase) tyrosine kinase. This compound is utilized in research to explore mechanisms of ALK-mediated oncogenesis and to evaluate the therapeutic efficacy of targeted treatments in malignancies such as non-small cell lung cancer. Its deuterium labeling allows for advanced studies in pharmacokinetics and metabolism, making it a valuable tool for chemical biology investigations.
  44. ALK Inhibitor

    ALK-IN-24 is a potent, orally active inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 value of 1.7 nM, also exhibiting inhibition of insulin receptor kinase with an IC50 value of 6 nM. It effectively suppresses the proliferation of lung adenocarcinoma cells and has demonstrated the ability to inhibit ALK-driven tumor growth in xenograft mouse models. This compound is applicable for research focused on non-small cell lung cancer and other ALK-related malignancies.
  45. ALK/IR/VEGFR2/TIE2/DLK Inhibitor

    CEP-14083 is an ATP-competitive inhibitor targeting ALK, with IC50 values of 2 nM in enzymatic assays. This compound also inhibits other kinases, including the insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2), and dual leucine zipper kinase (DLK). CEP-14083 has been shown to suppress CD274 mRNA expression and the function of NPM/ALK in NPM/ALK-positive T cell lymphoma cells. It is a valuable tool for research focused on lymphoma and related signaling pathways.
  46. ALK/EGFR Inhibitor

    ALK/EGFR-IN-1-d5 is a deuterated dual-target inhibitor that specifically targets ALK and EGFR, exhibiting IC50 values of 1.08 nM for EGFR and 2.395 nM for ALK. This compound effectively inhibits phosphorylated proteins within the EGFR, ALK, and BRK signaling pathways, disrupting the cell cycle and subsequently promoting apoptosis through a decrease in mitochondrial membrane potential. Furthermore, ALK/EGFR-IN-1-d5 shows significant anti-tumor activity in preclinical animal models, indicating its potential for advancing research in cancer therapeutics.
  47. ALK Inhibitor

    ALK-IN-22 is a potent inhibitor of Anaplastic Lymphoma Kinase (ALK), demonstrating IC50 values of 2.3 nM, 3.7 nM, and 2.9 nM against ALK, ALKL1196M, and ALKG1202R, respectively. This compound effectively down-regulates the phosphorylation of ALK and its downstream signaling proteins, thereby inducing apoptosis in tumor cells. ALK-IN-22 is suitable for various research applications, particularly in the study of tumors associated with ALK dysregulation.
  48. EML4-ALK PROTAC Degrader

    Pro-PEG3-BA is a targeted PROTAC degrader that specifically degrades EML4-ALK and EGFR mutants, with DC50 values of 0.42 μM and 13.50 μM, respectively. It effectively inhibits proliferation and induces cell cycle arrest and apoptosis in non-small cell lung cancer (NSCLC) cell lines in vitro. In vivo studies reveal that Pro-PEG3-BA rewires the ubiquitin-proteasome system, leading to a reduction in EML4-ALK protein levels while demonstrating a favorable safety profile. This reagent is suitable for research focused on non-small cell lung cancer treatments.
  49. ALK Inhibitor

    KF-20444 is a selective ALK inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent activity against ALK fusion proteins such as EML4-ALK and various ALK resistance mutations, including L1196M, G1202R, and F1174L. By inhibiting ALK phosphorylation in ALK-driven cancer cell lines, KF-20444 suppresses cell proliferation and promotes apoptosis. This compound shows significant anti-tumor efficacy in mouse models of ALK-positive non-small cell lung cancer (NSCLC) and neuroblastoma, making it a valuable tool for research on ALK-driven malignancies.
  50. ALK/c-Met/ROS1 Inhibitor

    Crizotinib acetate is an orally bioavailable inhibitor targeting ALK, c-Met, and ROS1 through ATP competition. It demonstrates potent inhibition of tyrosine phosphorylation in cell-based assays, with IC50 values of 20 nM for ALK, 8 nM for c-Met, 24 nM for NPM-ALK, and 11 nM for c-Met. The compound has shown significant efficacy in inhibiting tumor growth, making it a valuable tool in cancer research and therapeutic applications targeting these pathways.

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