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ALK

Items 1-50 of 142

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Catalog No.
Product Name
Application
Product Information
Citations
  1. A15801
    Entrectinib

    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.
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  2. A14213
    EW-7197 (Vactosertib)

    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
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  3. A16245
    Crizotinib hydrochloride

    c-Met/NPM-ALK inhibitor

    Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.
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  4. A11205
    LDN193189

    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.
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  5. A13450
    Brigatinib (AP26113)

    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.
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  6. A18000
    Alectinib Hydrochloride

    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.
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  7. A10712
    PF-2341066 (Crizotinib)

    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).
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  8. A12820
    DMH-1

    BMP inhibitor

    DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).
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  9. A11175
    GSK1838705A

    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.

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  10. A10662
    TAE684

    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).
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  11. A12358
    A 83-01

    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
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  12. A11134
    Alectinib (CH5424802)

    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.

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  13. A11157
    SB-505124

    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).
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  14. A11773
    ASP3026

    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.
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  15. A11948
    ALK-IN-1 (Brigatinib analog, AP26113 analog)

    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.

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  16. A13604
    ALK2-IN-2

    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.
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  17. A13744
    CEP-28122

    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.
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  18. A14207
    Lorlatinib (PF-06463922)

    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.

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  19. A14312
    WZ4003

    NUAK kinase inhibitor

    WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2
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  20. A14436
    A 77-01

    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.
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  21. A18457
    ALK-IN-6

    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.
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  22. A16096
    LDN-214117

    ALK2 inhibitor

    LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM.
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  23. A16207
    R-268712

    ALK5 inhibitor

    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
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  24. A16267
    HG-14-10-04

    ALK/EGFR inhibitor

    HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
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  25. A20919
    Belizatinib

    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.
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  26. A20971
    X-376

    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.
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  27. A19720
    Ensartinib

    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.
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  28. A19765
    SM 16

    ALK5/ALK4 inhibitor

    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
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  29. A20071
    WY-135

    ALK/ ROS1 dual inhibitor

    WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
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  30. A20077
    MS4077

    ALK PROTAC degrader

    MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37?nM for binding affinity to ALK.
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  31. A20089
    MS4078

    ALK PROTAC degrader

    MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19?nM for binding affinity to ALK.
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  32. A20205
    JH-VIII-157-02

    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.
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  33. A19269
    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.
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  34. A14987
    ALK inhibitor 1

    ALK inhibitor

    ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
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  35. A14988
    ALK inhibitor 2

    ALK inhibitor

    ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.
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  36. A15142
    LDK378 (Ceritinib) dihydrochloride

    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.
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  37. A15511
    KRCA-0008

    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.
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  38. A15543
    CEP-37440

    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).
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  39. A10827
    SB 525334

    ALK Inhibitor

    SB525334 is a selective inhibitor of transforming growth factor-β receptor I (ALK5, TGF-βRI) (IC50 = 14.3 nM). Inhibits TGF-β1-induced smad2/3 nuclear localization and TGF-βRI-induced mRNA expression in kidney cells
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  40. A30509
    APG-2449

    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.
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  41. A30753
    W23-1006

    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.
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  42. A33765
    Ceritinib-d7

    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.
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  43. A33776
    ALK-IN-24

    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.
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  44. A33804
    CEP-14083

    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.
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  45. A32707
    ALK/EGFR-IN-1-d5

    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.
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  46. A32728
    ALK-IN-22

    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.
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  47. A34327
    Crizotinib acetate

    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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  48. A34344
    CM-118

    c-Met/ALK Inhibitor

    CM-118 is a selective inhibitor of c-Met and ALK, targeting the HGF-induced c-Met phosphorylation and impairing ALK phosphorylation in key variants including EML4-ALKv1, ALK F1174L, and EML4-ALKv1 L1196M. With IC50 values of 0.92, 1.25, 1.9, and 3.5 μM respectively, CM-118 demonstrates significant anticancer activity against tumors reliant on c-Met or ALK oncogenic pathways. This compound is useful for investigating therapeutic strategies in cancers driven by these targets.
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  49. A34348
    SMU-B

    ALK Inhibitor

    SMU-B is a potent orally active inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of less than 0.5 nM, along with c-ros oncogene 1 (ROS1) and c-MET, exhibiting IC50 values of 1.87 nM and 28.9 nM for AXL. This compound demonstrates significant antiproliferative activity against MKN45, H1993, and H441 cell lines, with IC50s of 0.02 μM, 1.58 μM, and 2.82 μM, respectively. Additionally, SMU-B has shown promising antitumor efficacy in various mouse models, highlighting its potential for cancer research applications.
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  50. A34379
    Crizotinib-d8

    Stable Isotope

    Crizotinib-d8 is a deuterated analog of Crizotinib, functioning as an ATP-competitive inhibitor of ALK and c-Met. This compound exhibits potent biological activity, with IC50 values of 20 nM and 8 nM, respectively, and effectively inhibits tyrosine phosphorylation of NPM-ALK and c-Met in cellular assays. Additionally, Crizotinib-d8 serves as an inhibitor of ROS1. This stable isotope is primarily utilized in pharmacokinetic studies and metabolic research involving Crizotinib to enhance understanding of its therapeutic mechanisms.
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