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ALK

Anaplastic lymphoma kinase (ALK) also known as ALK tyrosine kinase receptor or CD246 (cluster of differentiation 246) is an enzyme that in humans is encoded by the ALK gene.

  • A 83-01
    T3031909910-43-6
    A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.
    • $52
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  • SB-431542
    T1726301836-41-9
    SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.
    • $50
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  • Ceritinib
    T17911032900-25-6
    Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM).
    • $45
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  • CEP-28122 mesylate salt (1022958-60-6 free base)
    T10759
    CEP-28122 mesylate salt (1022958-60-6 free base) is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay).
    • $66
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  • LDN-193189 HCl
    T61581062368-62-0
    LDN-193189 HCl (LDN193189 Hydrochloride) is a selective BMP type I receptor kinases inhibitor.
    • $37
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    TargetMol | Citations Cited
  • N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-bromoaniline
    T98371352608-94-6In house
    Compound 12d is a potent ALK5 inhibitor with an IC50 of 7nM.
    • $148
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  • 5-phenylthieno[2,3-d]pyrimidin-4-amine
    T50042195193-10-3
    5-phenylthieno[2,3-d]pyrimidin-4-amine is a heterocyclic compound. It inhibits a variety of enzymes such as kinases and phosphodiesterases and has potential therapeutic activity for a variety of diseases.
    • $45
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  • CH5424802 analog
    T92241256577-71-5
    CH5424802 analog is a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.
    • $133
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  • Conteltinib
    T149971384860-29-0In house
    Conteltinib (CT-707) is an enzyme inhibitor with antitumor activity targeting FAK, ALK, and Pyk2.Conteltinib exhibits significant inhibition of FAK, overcomes hypoxia-mediated sorafenib resistance in hepatocellular carcinoma through inhibition of YAP signaling, and can be used in advanced ALK-positive non-small-cell lung cancer and lymphoma.
    • $100
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  • ALK2-IN-2
    T102872254409-25-9In house
    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) (IC50: 9 nM), inhibiting ALK2 700-fold more than ALK3.
    • $93
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  • GW-6604
    T9947452342-37-9In house
    GW-6604 is an ALK5 inhibitor and shows clear antifibrotic effects resulting in liver function improvement.
    • $30
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  • EML4-ALK kinase inhibitor 1
    T111841373409-08-5In house
    EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
    • $88
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  • KER047
    T397642248154-85-8In house
    KER047 (ALK2-IN-4) is an ALK2 inhibitor with potential anticancer activity and can be used in the study of non-small cell lung cancer.
    • $97 TargetMol
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  • LDN-212854
    T19001432597-26-6
    LDN-212854 (BMP Inhibitor III), a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus ALK1/3 compared to other inhibitors.
    • $42
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  • Repotrectinib
    T40711802220-02-5
    Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.
    • $45
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  • SB-505124
    T2462694433-59-5
    SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
    • $34
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  • Alectinib
    T19361256580-46-7
    Alectinib (RG-7853) is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity.
    • $39
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  • Crizotinib
    T1661877399-52-5
    Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinases inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptor.
    • $46
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  • SB 525334
    T1763356559-20-1
    SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
    • $53
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  • Belizatinib
    T42571357920-84-3
    Belizatinib (TSR-011) is an effective, oral and dual inhibitor of ALK (IC50: 0.7 nM, wild-type recombinant ALK) and TRKA, TRKB, and TRKC.
    • $36
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  • Lorlatinib
    T30611454846-35-5
    Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
    • $35
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  • LDN193189
    T19351062368-24-4
    LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8/0.8/5.3/16.7 nM for ALK1/2/3/6).
    • $41
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  • DMH-1
    T19421206711-16-1
    DMH-1 is a potent and selective BMP inhibitor.
    • $53
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  • Entrectinib
    T36781108743-60-7
    Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.
    • $35
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  • Brigatinib
    T36211197953-54-0
    Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor.
    • $30
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  • Vactosertib
    T64961352608-82-2
    Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.
    • $39
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  • RepSox
    T6337446859-33-2
    RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells.
    • $30
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  • ALK-IN-26
    T777542447607-85-2
    ALK-IN-26 is an ALK inhibitor with potential anticancer activity.ALK-IN-26 shows antiproliferative activity against glioblastoma.ALK-IN-26 induces apoptosis, autophagy and necrosis.
    • $35
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  • Ascrinvacumab
    T768581463459-96-2
    Ascrinvacumab (PF-03446962) is a highly humanized IgG2 monoclonal antibody against ALK-1. Ascrinvacumab has a Kd value of 7 nM for human ALK1. Ascrinvacumab has an inhibitory effect on TGF-β and can be used to study hepatocellular carcinoma (HCC).
    • $247
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  • MS4077
    T137812230077-10-6
    MS4077 is an degrader of anaplastic lymphoma kinase (ALK) PROTAC(Kd of 37 nM for binding affinity to ALK).
    • $871
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  • F-1
    T112542244775-31-1
    F-1 is IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways.
    • $111
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  • BIBF0775
    T5197334951-90-5
    BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
    • $60
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  • CEP-37440
    T26551391712-60-9
    CEP-37440 is an effective and specific Dual FAK/ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK).
    • $31
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  • Ensartinib hydrochloride
    T223242137030-98-7
    Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.
    • $60
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  • ALK inhibitor 1
    T10285761436-81-1
    ALK inhibitor 1 is a selective ALK kinase inhibitor.
    • $80
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  • ASP3026
    T19621097917-15-1
    ASP3026 has been used in trials studying the treatment of Solid Tumor, B-Cell Lymphoma, Advanced Malignancies, Positive for Anaplastic Lymphoma Kinase, and Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS.
    • $35
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  • A 83-01 sodium salt
    T104422828431-89-4
    A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC 50 s of 12 nM, 45 nM and 7.5 nM against the ALK5, ALK4 and ALK7 induced transcription, respectively [1].
    • $4,249
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  • KRCA-0008
    T26411472795-20-2
    KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability.
    • $39
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  • MS4078
    T161532229036-62-6
    MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.
    • $44
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  • JH-VIII-157-02
    T156121639422-97-1
    JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L.
    • $118
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  • HG-14-10-04
    T40151356962-34-9
    HG-14-10-04 is a potent and specific ALK inhibitor.
    • $55
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  • ML347
    T19431062368-49-3
    ML347 (LDN 193719)(DN193719) is a highly specific ALK1/2 inhibitor ( IC50: 46/32 nM), and the selectivity for ALK2 is >300-fold than ALK3.
    • $33
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  • IN-1130
    T15572868612-83-3
    IN-1130 is a selective inhibitor of ALK5 with IC50 values of 5.3 nM, 36 nM, and 4.3 μM for phosphorylation of ALK5-mediated Smad3, ALK5 phosphorylation of casein and p38α mitogen-activated protein kinase.
    • $48
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  • LDN-214117
    T19441627503-67-6
    LDN-214117 is a potent and selective ALK2 inhibitor.
    • $33
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  • Vactosertib Hydrochloride
    T152621352610-25-3
    Vactosertib Hydrochloride is an orally active and ATP-competitive ALK5 inhibitor (IC50: 12.9 nM). It has potently antimetastatic activity and anticancer effect. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50: 17.3 nM).
    • $67
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  • K02288
    T19141431985-92-0
    K 02288 is a novel small molecule inhibitor of ALK1/2/3/6.
    • $33
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  • R-268712
    T16708879487-87-3
    R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.
    • $44
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  • Ceritinib dihydrochloride
    T1791L1380575-43-8
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive inhibitor of ALK tyrosine kinase(IC50 of 200 pM), and also inhibits IGF-1R, InsR, and STK22D (IC50 values of 8, 7, and 23 nM, respectively), shows great antitumor potency
    • $43
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  • GSK1838705A
    T30791116235-97-2
    GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases.
    • $34
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  • AZ 12799734
    T358961117684-36-2
    AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.
    • $113
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