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  • Protein Tyrosine Kinases

Protein Tyrosine Kinases

Items 1-50 of 1870

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  1. A10108
    Saracatinib (AZD0530)

    Src/Abl inhibitor

    Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively.
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  2. 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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  3. A12694
    Pacritinib (SB1518)

    JAK2/FLT3 inhibitor

    Pacritinib, also known as SB1518, is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis.
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  4. A10001
    Sorafenib Tosylate (Nexavar)

    Raf inhibitor

    Sorafenib Tosylate (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
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  5. A10699
    Pazopanib HCl (GW786034)

    VEGFR/PDGFR/FGFR inhibitor

    Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
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  6. A10967
    Vatalanib (PTK787) 2HCl

    VEGFR inhibitor

    Vatalanib (PTK787 or PTK/ZK) is a small molecule protein kinase inhibitor that inhibits angiogenesis that inhibits all known VEGF receptors, as well as platelet-derived growth factor receptor-beta and c-kit, but is most selective for VEGFR-2. CAS: 212141-51-0 (HCl) 212141-54-3 (Free base)
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  7. A11496
    Motesanib (AMG706)

    VEGFR Inhibitor

    Motesanib (AMG706) is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors with IC?? values of 2 nM (VEGFR1), 3 nM (VEGFR2), 6 nM (VEGFR3), 84 nM (PDGFR), and 8 nM (Kit).
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  8. A10953
    TSU-68 (Orantinib, SU6668)

    PDFGRβ inhibitor

    Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
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  9. A10963
    Vandetanib (ZD6474)

    VEGFR inhibitor

    Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
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  10. A10254
    Brivanib (BMS-540215)

    VEGFR-2 inhibitor

    Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.
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  11. A10025
    Linifanib (ABT-869)

    VEGFR/PDGFR inhibitor

    Linifanib (ABT-869) is a structurally novel, potent inhibitor of RTK, VEGF and PDGF with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGFR-β, KDR, and CSF-1R, respectively.

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  12. A10185
    Cediranib (AZD2171)

    VEGFR inhibitor

    Cediranib (AZD2171) is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.
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  13. A10101
    Tivozanib (AV-951)

    VEGFR Inhibitor

    Tivozanib (AV-951) is an oral VEGF receptor tyrosine kinase inhibitor that is designed to inhibit all three VEGF receptors.
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  14. A10998
    Foretinib (GSK1363089, XL880)

    c-MET inhibitor

    Foretinib (GSK1363089), a multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces Anoikis, and impairs ovarian cancer metastasis.
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  15. A10426
    Genistin (Genistoside)
    Genistin is an isoflavone found in a number of dietary plants like soy and kudzu. It was shown to stimulate estrogen-dependent breast cancer cell growth in vivo.
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  16. A10043
    AEE788

    EGFR inhibitor

    AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2.
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  17. 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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  18. A16245
    Crizotinib hydrochloride

    c-Met/NPM-ALK inhibitor

    Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.
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  19. A10703
    PD173074

    FGFR1/VEGFR2 Inhibitor

    PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR.
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  20. A15271
    Vandetanib HCl

    VEGFR inhibitor

    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
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  21. A11021
    NVP-AEW541

    IGF-1R inhibitor

    NVP-AEW541 is a selective IGF-1R kinase inhibitor that inhibits the autophosphorylation activity of IGF-1R (IC50 = 0.086 uM) and prevents IGF-1-mediated survival and proliferation of MCF-7 cells (IC50 = 0.16 and 1.64 uM, respectively).
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  22. A10211
    Canertinib (CI-1033)

    HER2/ErbB2 inhibitor

    Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).
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  23. A11768
    Radicicol

    Hsp90/SRC/COX-2 Inhibitor

    Radicicol is a potent inhibitor of Hsp90, SRC, and Cox-2
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  24. A11158
    ARRY334543 (Varlitinib)

    EGFR inhibitor

    ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2.
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  25. A11416
    Erlotinib

    EGFR inhibitor

    Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.
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  26. A10422
    Gefitinib (Iressa)

    EGFR Inhibitor

    Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.
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  27. A12723
    PP2

    Src Inhibitor

    PP2 is a selective inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 4 and 5 nM respectively). Displays > 10000-fold selectivity over ZAP-70 and JAK2. Moderately inhibits CSK (IC50 = 0.73 μM).
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  28. A10290
    Dasatinib (BMS-354825)

    Abl-Src inhibitor

    Dasatinib (BMS-354825) is an oral multi- BCR/ABL and Src family tyrosine kinase inhibitor. The main targets of dasatinib, are BCR/ABL, Src, c-Kit, ephrin receptors, and several other tyrosine kinases, but not erbB kinases such as EGFR or Her2.
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  29. A14143
    UNC 2250

    Selective Mer Kinase inhibitor

    UNC2250 is a potent and selective Mer Kinase inhibitor.
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  30. A18014
    Afatinib

    EGFR inhibitor

    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
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  31. A10468
    Imatinib Mesylate

    Bcr-Abl inhibitor

    Imatinib mesylate, a selective tyrosine kinase inhibitor, induced a sustained objective response in treating gastrointestinal stromal tumors with the inhibition of the KIT signal-transduction pathway.
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  32. A16320
    Dasatinib Monohydrate
    Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
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  33. A12557
    LY2801653 (Merestinib)

    c-MET inhibitor

    LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).
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  34. A15152
    Masitinib mesylate

    KIT/PDGFR inhibitor

    Masitinib mesylate is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.
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  35. A11350
    CP-673451

    PDGFRα/β inhibitor

    CP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM.
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  36. A10658
    NVP-ADW742

    IGF-1R inhibitor

    NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM.
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  37. A10893
    Taxifolin

    VEGFR-2 Inhibitor

    Taxifolin is found to bind at the ATP-binding site on VEGFR-2 kinase with large value of binding energy and act as type I competitive inhibitor.
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  38. A11022
    AG-1478 (Tyrphostin AG-1478)

    EGFR Inhibitor

    AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM.
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  39. A10502
    Ki8751

    VEGFR-2 inhibitor

    Ki8751 is a cell-permeable quinolyloxyphenyl-urea compound that acts as a Flk-1 (VEGFR-2)-selective inhibitior in both cell-based and cell-free assays.
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  40. A11518
    Pazopanib (GW-786034)

    VEGFR inhibitor

    Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
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  41. A11028
    AV-412

    EGFR inhibitor

    AV-412 is an EGFR/HER2 inhibitor that binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis.
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  42. 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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  43. A10161
    Bosutinib (SKI-606)

    Src inhibitor

    Bosutinib (SKI-606) is a tyrosine kinase inhibitor undergoing research for use in the treatment of cancer.
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  44. A11059
    BMS-754807

    IGF-1R inhibitor

    BMS-754807 is an efficacious, orally active growth factor 1 receptor/insulin receptor family-targeted kinase inhibitor that may act in combination with a wide array of established anticancer agents.
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  45. A15848
    FIIN-3

    Irreversible FGFR inhibitor

    FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor.
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  46. A10250
    Regorafenib (BAY 73-4506)

    VEGFR inhibitor

    Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
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  47. A11132
    Capmatinib (INCB28060)

    c-MET Inhibitor

    INCB28060, a novel inhibitor of c-MET kinase. INCB28060 exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines.
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  48. A13573
    PP1 Analog II, 1NM-PP1
    PP1 Analog II, 1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.
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  49. A11400
    AG-1024 (Tyrphostin)

    IGF-1R Inhibitor

    AG-1024 (Tyrphostin) is a specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor tyrosine kinase activity. Exhibits lower IC50 values for IGF-1 than for the insulin receptor. Also inhibits insulin-stimulated cellular proliferation.
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  50. A20550
    Futibatinib

    FGFR inhibitor

    Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor.
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  1. Inhibitor 1597items
  2. Agonist 3items
  3. Antagonist 4items
  4. Activator 3items
  5. Modulator 2items
  6. Blocker 1item
  7. Degrader 3items
  8. Stimulator 1item
Target
  1. HDAC 1item
  2. HDAC1 1item
  3. HDAC2 1item
  4. HDAC3 1item
  5. HDAC4 1item
  6. HDAC5 1item
  7. HDAC6 1item
  8. HDAC7 1item
  9. HDAC8 1item
  10. HDAC9 1item
  11. HDAC10 1item
  12. EGFR/ErbB1/HER1 15items
  13. ErbB2/HER2 7items
  14. ErbB4/HER4 1item
  15. JAK1 1item
  16. JAK2 7items
  17. JAK3 4items
  18. Tyk2 1item
  19. STAT3 1item
  20. CDK2 2items
  21. FLT3 3items